Certain chemical entities, compositions, and methods

ABSTRACT

Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

CROSS-REFERENCE

This application is a continuation of U.S. application Ser. No.15/586,710, filed May 4, 2017, now U.S. Pat. No. 10,487,108, issued Nov.26, 2019, which is a continuation of U.S. application Ser. No.14/397,845, filed Oct. 29, 2014, now U.S. Pat. No. 9,676,813, issuedJun. 13, 2017, which is a U.S. National Stage Entry of InternationalApplication No. PCT/US2013/038705, filed Apr. 29, 2013, which claimspriority from U.S. Provisional application No. 61/639,930, filed Apr.29, 2012, all of which are incorporated herein by reference in theirentirety.

BACKGROUND

Cancer can be viewed as a breakdown in the communication between tumorcells and their environment, including their normal neighboring cells.Signals, both growth-stimulatory and growth-inhibitory, are routinelyexchanged between cells within a tissue. Normally, cells do not dividein the absence of stimulatory signals, and likewise, will cease dividingin the presence of inhibitory signals. In a cancerous, or neoplasticstate, a cell acquires the ability to “override” these signals and toproliferate under conditions in which normal cells would not grow.

Cardiotonic steroids like digoxin and digitoxin are a class of naturallyderived compounds that bind to and inhibit Na⁺/K⁺-ATPase (sodium pump).Members of this family have been used for the treatment of heart failureand arrhythmia for many years. Recent findings have revealed that thesecompounds may be involved in the regulation of several importantcellular processes. Several cardiotonic steroids such as digitoxin andoleandrin have shown inhibitory effect on the growth of human tumorcells.

SUMMARY OF THE INVENTION

In an aspect, the invention provides least one chemical entity chosenfrom compounds of Formula I

and pharmaceutically acceptable salts thereof, whereinR₁, R₂, R₃, R₄, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independently chosenfrom hydrogen, hydroxy, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, optionallysubstituted alkynyl, optionally substituted alkoxy, optionallysubstituted aryloxy, optionally substituted heteroaryloxy, optionallysubstituted heterocycloalkyloxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino; orR₁ and R₂, or R₅ and R₆, or R₇ and R₈, or R₉ and R₁₀, or R₁₁ and R₁₂mutually independently, together in each case denote an oxo group (═O);orR₄ and R₅ may optionally be joined together with any intervening atomsto form an optionally substituted heterocycloalkyl ring;R₇ is chosen from hydrogen, hydroxy, optionally substituted alkoxy,optionally substituted aryloxy, optionally substituted heteroaryloxy,optionally substituted heterocycloalkyloxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino;R₈ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, and optionallysubstituted alkynyl;R₁₃ is chosen from hydrogen, optionally substituted alkyl, and formyl;R₁₄ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; andR₁₅ is chosen from hydrogen, hydroxyl, formyl, optionally substitutedalkoxy, optionally substituted alkyl, optionally substituted cycloalkyl,optionally substituted heterocycloalkyl, optionally substituted aryl,and optionally substituted heteroaryl, —COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈,—C(NR₁₉)NR₁₇R₁₈, —C(NCN)NR₁₇R₁₈, —SO₂R₁₆, and —SO₂NR₁₇R₁₈, where R₁₆ ischosen from optionally substituted alkyl, optionally substitutedcycloalkyl, optionally substituted heterocycloalkyl, optionallysubstituted aryl, and optionally substituted heteroaryl; and R₁₇, R₁₈and R₁₉ are independently chosen from hydrogen, optionally substitutedalkyl, optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl; or R₁₇ and R₁₈ may be joined together with anyintervening atoms to form an optionally substituted heterocycloalkylring; orR₁₄ and R₁₅ are joined together with any intervening atoms to form anoptionally substituted 4- to 8-membered heterocycloalkyl or optionallysubstituted 5- to 8-membered heteroaryl ring;W₁ is chosen from the following moieties:

wherein Y is chosen from O and NR₂₁;R₂₀ is chosen from cyano, halo, hydroxy, azido, nitro, carboxy,sulfinyl, sulfanyl, optionally substituted alkoxy, optionallysubstituted aryloxy, optionally substituted heteroaryloxy, optionallysubstituted heterocycloalkyloxy, optionally substituted alkoxycarbonyl,optionally substituted alkyl, optionally substituted alkenyl, optionallysubstituted aryloxy, optionally substituted aryl, optionally substitutedheteroaryl, optionally substituted heterocycloalkyl, optionallysubstituted amino, optionally substituted acyl, optionally substitutedalkoxycarbonyl, optionally substituted aminocarbonyl, optionallysubstituted aminosulfonyl, optionally substituted carbaminodoyl, andoptionally substituted alkynyl;R₂₁ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl;W₂ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, and optionallysubstituted alkynyl;m is selected from 0, 1, 2, and 3;n, p, and q is independently selected from 0 and 1; andthe dotted line represents a single bond or a double bond.

In some embodiments, R₁, R₂, R₃, R₄, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ areindependently chosen from hydrogen, hydroxy, optionally substitutedalkyl, optionally substituted alkoxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino. In some cases, R₁,R₂, R₃, R₄, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independently chosen fromhydrogen, hydroxy, and optionally substituted alkyl. For example, R₁,R₂, R₃, R₄, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independently chosen fromhydrogen, hydroxy, and methyl. In some cases, R₄ is hydroxy.

In some embodiments, the invention provides a compound of Formula I,wherein R₄ and R₅ are joined together with any intervening atoms to forman optionally substituted 3- to 8-membered heterocycloalkyl ring. Forexample, R₄ and R₅ are joined together with any intervening atoms toform an oxirane ring.

In some embodiments, R₇ is chosen from hydrogen, hydroxy, optionallysubstituted alkoxy, optionally substituted aminocarbonyloxy, optionallysubstituted acyloxy, optionally substituted alkoxycarbonyloxy, andoptionally substituted amino. In some cases, R₇ is chosen from hydrogenand optionally substituted acyloxy. For example, R₇ is chosen fromhydrogen and —OCOCH₃.

In some embodiments, R₈ and W₂ are independently chosen from hydrogenand optionally substituted alkyl.

In some embodiments, R₁₃ is chosen from hydrogen and optionallysubstituted alkyl. In some cases, R₁₃ is chosen from hydrogen andoptionally substituted alkyl. For example, R₁₃ is chosen from hydrogen,methyl, and hydroxymethyl.

In some embodiments, Y is chosen from O, NH and NCH₃. For example Y isO.

In some embodiments, R₂₀ is chosen from cyano, halo, hydroxy, carboxy,sufonyl, optionally substituted alkoxy, optionally substitutedalkoxycarbonyl, optionally substituted alkyl, optionally substitutedamino, optionally substituted acyl, optionally substitutedalkoxycarbonyl, optionally substituted aminocarbonyl, and optionallysubstituted aminosulfonyl.

In some examples, m is 0.

In some cases, the dotted line represents a single bond. In someexamples, the dotted line represents a double bond.

In some embodiments, the compound of Formula I has the formula:

In other embodiments, the compound of Formula I has the formula:

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ia.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ib.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ic.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Id.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ie.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula If.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ig.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ih.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ii.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ij.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula Ik.

In some embodiments, the compound of Formula I is chosen from compoundsof Formula

In some embodiments, the R₁₄ in Formula I (Ia-Il) is chosen fromhydrogen, optionally substituted lower alkyl, optionally substitutedcycloalkyl, optionally substituted heterocycloalkyl, optionallysubstituted aryl, and optionally substituted heteroaryl. In some cases,R₁₄ is chosen from hydrogen and optionally substituted lower alkyl. Forexample, R₁₄ is hydrogen. In some cases R₁₄ is not hydrogen. Forexample, R₁₄ is optionally substituted alkyl, optionally substitutedcycloalkyl, or optionally substituted heterocycloalkyl.

In some embodiments, the R₁₅ in Formula I (Ia-Il) is chosen fromhydrogen, optionally substituted alkyl, optionally substitutedcycloalkyl, optionally substituted heterocycloalkyl, —COR₁₆, —CO₂R₁₆,—CONR₁₇R₁₈, —C(NR₁₉)NR₁₇R₁₈, —C(NCN)NR₁₇R₁₈, —SO₂R₁₆, and —SO₂NR₁₇R₁₈.In some cases, R₁₅ is chosen from —COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈, and—SO₂NR₁₇R₁₈. For example, R₁₅ is chosen from —COR₁₆, —CO₂R₁₆, and—CONR₁₇R₁₈.

In some embodiments, R₁₄ and R₁₅ are not hydrogen. In some embodiments,R₁₄ is optionally substituted alkyl, optionally substituted cycloalkyl,or optionally substituted heterocycloalkyl. In other embodiments, R₁₅ is—COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈, —C(NR₁₉)NR₁₇R₁₈, —C(NCN)NR₁₇R₁₈, —SO₂R₁₆,and —SO₂NR₁₇R₁₈. In some embodiments, R₁₅ is SO₂R₁₆, —COR₁₆, or —CO₂R₁₆.

In some embodiments, R₁₄ and R₁₅ are joined together with anyintervening atoms to form an optionally substituted 4- to 8-memberedheterocycloalkyl or optionally substituted 5- to 8-membered heteroarylring. For example, R₁₄ and R₁₅ form an optionally substituted 5- or6-membered heterocycloalkyl ring. The 5- or 6-membered heterocycloalkylring may be, for example, a morpholino, piperazino, or pyrrolidinogroup.

In some embodiments, R₁₆ is chosen from optionally substituted alkyl,optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl; R₁₇ and R₁₈ are independently chosen fromhydrogen, optionally substituted alkyl, optionally substitutedcycloalkyl, optionally substituted heterocycloalkyl, optionallysubstituted aryl, and optionally substituted heteroaryl; and R₁₉ ischosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, and optionally substituted heterocycloalkyl. Forexample, R₁₆ is chosen from optionally substituted alkyl, optionallysubstituted cycloalkyl, and optionally substituted heterocycloalkyl; R₁₇and R₁₈ are independently chosen from hydrogen, optionally substitutedalkyl, optionally substituted cycloalkyl, and optionally substitutedheterocycloalkyl; and R₁₉ is chosen from hydrogen and optionallysubstituted alkyl.

In some embodiments R₁₇ and R₁₈ may be joined together with anyintervening atoms to form an optionally substituted 4- to 8-memberedheterocycloalkyl ring. In some cases, R₁₇ and R₁₈ are joined together toform a 4- to 8-membered heterocycloalkyl ring optionally substitutedwith one or two groups independently chosen from amino, hydroxyl, oxo,and lower alkyl. For example, R₁₇ and R₁₈ is joined together to form a5- to 7-membered heterocycloalkyl ring chosen from3-hydroxypyrrolidine-1-yl, 3-aminopyrrolidine-1-yl,3-oxopiperazine-1-yl, 4-methyl-1,4-diazepane-1-yl, 1,4-diazepane-1-yl,piperazine-1-yl, 4-methylpiperazine-1-yl, and morpholine-4-yl.

In some embodiments, R₁₄ and R₁₅ are joined together with anyintervening atoms to form an optionally substituted 4- to 8-memberedheterocycloalkyl ring.

In another aspect, the invention provides a pharmaceutical compositioncomprising a pharmaceutically acceptable carrier and at least onechemical entity of Formula I (Ia-Il). The pharmaceutical composition ofthe invention may be formulated in a form of tablets, capsules, powders,liquids, suspensions, suppositories, or aerosols. The invention alsoprovides packaged pharmaceutical compositions comprising apharmaceutical composition of the invention and instructions for usingthe composition to treat a subject suffering from cancer.

In another aspect, the invention provides a method of treating cancer ina subject. The methods of the invention comprise administering to asubject in need thereof a therapeutically effective amount of at leastone chemical entity of the invention (Formula I (Ia-Il)).

DETAILED DESCRIPTION OF THE INVENTION

Provided are certain chemical entities and compositions thereof that maybe useful in the treatment of cancer.

Provided is at least one chemical entity chosen from compounds ofFormula I

and pharmaceutically acceptable salts thereof, wherein

R₁, R₂, R₃, R₄, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independently chosenfrom hydrogen, hydroxy, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, optionallysubstituted alkynyl, optionally substituted alkoxy, optionallysubstituted aryloxy, optionally substituted heteroaryloxy, optionallysubstituted heterocycloalkyloxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino; or

R₁ and R₂, or R₅ and R₆, or R₇ and R₈, or R₉ and R₁₀, or R₁₁ and R₁₂mutually independently, together in each case denote an oxo group (═O);or

R₄ and R₅ may optionally be joined together with any intervening atomsto form an optionally substituted heterocycloalkyl ring;

R₇ is chosen from hydrogen, hydroxy, optionally substituted alkoxy,optionally substituted aryloxy, optionally substituted heteroaryloxy,optionally substituted heterocycloalkyloxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino;

R₈ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, and optionallysubstituted alkynyl;

R₁₃ is chosen from hydrogen, optionally substituted alkyl, and formyl;

R₁₄ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; and

R₁₅ is chosen from hydrogen, hydroxyl, formyl, optionally substitutedalkoxy, optionally substituted alkyl, optionally substituted cycloalkyl,optionally substituted heterocycloalkyl, optionally substituted aryl,and optionally substituted heteroaryl, —COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈,—C(NR₁₉)NR₁₇R₁₈, —C(NCN)NR₁₇R₁₈, —SO₂R₁₆, and —SO₂NR₁₇R₁₈, where R₁₆ ischosen from optionally substituted alkyl, optionally substitutedcycloalkyl, optionally substituted heterocycloalkyl, optionallysubstituted aryl, and optionally substituted heteroaryl; and R₁₇, R₁₈and R₁₉ are independently chosen from hydrogen, optionally substitutedalkyl, optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl; or R₁₇ and R₁₈ may be joined together with anyintervening atoms to form an optionally substituted heterocycloalkylring, or

R₁₄ and R₁₅ are joined together with any intervening atoms to form anoptionally substituted 4- to 8-membered heterocycloalkyl or optionallysubstituted 5- to 8-membered heteroaryl ring;

W₁ is chosen from the following moieties:

wherein Y is chosen from O and NR₂₁;

R₂₀ is chosen from cyano, halo, hydroxy, azido, nitro, carboxy,sulfinyl, sulfanyl, optionally substituted alkoxy, optionallysubstituted aryloxy, optionally substituted heteroaryloxy, optionallysubstituted heterocycloalkyloxy, optionally substituted alkoxycarbonyl,optionally substituted alkyl, optionally substituted alkenyl, optionallysubstituted aryloxy, optionally substituted aryl, optionally substitutedheteroaryl, optionally substituted heterocycloalkyl, optionallysubstituted amino, optionally substituted acyl, optionally substitutedalkoxycarbonyl, optionally substituted aminocarbonyl, optionallysubstituted aminosulfonyl, optionally substituted carbaminodoyl, andoptionally substituted alkynyl;

R₂₁ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl;

W₂ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, and optionallysubstituted alkynyl;

m is selected from 0, 1, 2, and 3;

n, p, and q is independently selected from 0 and 1; and

the dotted line represents a single bond or a double bond.

Also provided is a pharmaceutical composition comprising apharmaceutically acceptable carrier and at least one chemical entitydescribed herein.

Also provided is a packaged pharmaceutical composition comprising apharmaceutical composition described herein and instructions for usingthe composition to treat a subject suffering from cancer.

Also provided is a method of treating cancer in a subject whichcomprises administering to a subject in need thereof a therapeuticallyeffective amount of at least one chemical entity described herein.

As used herein, the following words and phrases are generally intendedto have the meanings as set forth below, except to the extent that thecontext in which they are used indicates otherwise.

The following abbreviations and terms have the indicated meaningsthroughout:

-   AcOH=acetic acid-   Boc=tert-butoxycarbonyl-   c-=cyclo-   DCC=dicyclohexylcarbodiimide-   DCM=dichloromethane-   DIEA=N,N-diisopropylethylamine-   DMAP=4-dimethylaminopyridine-   EDC=1-ethyl-3-(3-dimethylaminopropyl) carbodiimide-   eq=equivalent(s)-   Et=ethyl-   EtOAc or EA=ethyl acetate-   EtOH=ethanol-   g=gram-   h or hr=hour-   HBTU=O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium    hexafluorophosphate-   HOBt=hydroxybenzotriazole-   HPLC=high pressure liquid chromatography-   i-=iso-   kg or Kg=kilogram-   L or l=liter-   LC/MS=LCMS=liquid chromatography-mass spectrometry-   LRMS=low resolution mass spectrometry-   m/z=mass-to-charge ratio-   Me=methyl-   MeOH=methanol-   mg=milligram-   min=minute-   mL=milliliter-   mmol=millimole-   n-=normal-   NaOAc=sodium acetate-   PE=petroleum ether-   Ph=phenyl-   Prep=preparative-   quant.=quantitative-   RP-HPLC=reverse phase-high pressure liquid chromatography-   rt or RT=room temperature-   s-=sec-=secondary-   t-=tert-=tertiary-   THF=tetrahydrofuran-   TLC=thin layer chromatography-   UV=ultraviolet

As used herein, when any variable occurs more than one time in achemical formula, its definition on each occurrence is independent ofits definition at every other occurrence.

As used herein, a dash (“-”) that is not between two letters or symbolsis used to indicate a point of attachment for a substituent. Forexample, —CONH₂ is attached through the carbon atom.

As used herein, “optional” or “optionally” is meant that thesubsequently described event or circumstance may or may not occur, andthat the description includes instances wherein the event orcircumstance occurs and instances in which it does not. For example,“optionally substituted alkyl” encompasses both “alkyl” and “substitutedalkyl” as defined below. It will be understood by those skilled in theart, with respect to any group containing one or more substituents, thatsuch groups are not intended to introduce any substitution orsubstitution patterns that are sterically impractical, syntheticallynon-feasible and/or inherently unstable.

As used herein, “alkyl” refers to straight chain and branched chainhaving the indicated number of carbon atoms, usually from 1 to 20 carbonatoms, for example 1 to 8 carbon atoms, such as 1 to 6 carbon atoms. Forexample C₁-C₆ alkyl encompasses both straight and branched chain alkylof from 1 to 6 carbon atoms. When an alkyl residue having a specificnumber of carbons is named, all branched and straight chain versionshaving that number of carbons are intended to be encompassed; thus, forexample, “butyl” is meant to include n-butyl, sec-butyl, isobutyl andt-butyl; “propyl” includes n-propyl and isopropyl. “Lower alkyl” refersto alkyl groups having one to six carbons. Examples of alkyl groupsinclude methyl, ethyl, propyl, isopropyl, n-butyl, sec-butyl,tert-butyl, pentyl, 2-pentyl, isopentyl, neopentyl, hexyl, 2-hexyl,3-hexyl, 3-methylpentyl, and the like. Alkylene is a subset of alkyl,referring to the same residues as alkyl, but having two points ofattachment. Alkylene groups will usually have from 2 to 20 carbon atoms,for example 2 to 8 carbon atoms, such as from 2 to 6 carbon atoms. Forexample, C₀ alkylene indicates a covalent bond and C₁ alkylene is amethylene group.

As used herein, “alkenyl” refers to an unsaturated branched orstraight-chain alkyl group having at least one carbon-carbon double bondderived by the removal of one molecule of hydrogen from adjacent carbonatoms of the parent alkyl. The group may be in either the cis or transconfiguration about the double bond(s). Typical alkenyl groups include,but are not limited to, ethenyl; propenyls such as prop-1-en-1-yl,prop-1-en-2-yl, prop-2-en-1-yl (allyl), prop-2-en-2-yl; butenyls such asbut-1-en-1-yl, but-1-en-2-yl, 2-methyl-prop-1-en-1-yl, but-2-en-1-yl,but-2-en-1-yl, but-2-en-2-yl, buta-1,3-dien-1-yl, buta-1,3-dien-2-yl;and the like. In certain embodiments, an alkenyl group has from 2 to 20carbon atoms and in other embodiments, from 2 to 6 carbon atoms. “Loweralkenyl” refers to alkenyl groups having two to six carbons.

As used herein, “alkynyl” refers to an unsaturated branched orstraight-chain alkyl group having at least one carbon-carbon triple bondderived by the removal of two molecules of hydrogen from adjacent carbonatoms of the parent alkyl. Typical alkynyl groups include, but are notlimited to, ethynyl; propynyls such as prop-1-yn-1-yl, prop-2-yn-1-yl;butynyls such as but-1-yn-1-yl, but-1-yn-3-yl, but-3-yn-1-yl; and thelike. In certain embodiments, an alkynyl group has from 2 to 20 carbonatoms and in other embodiments, from 3 to 6 carbon atoms. “Loweralkynyl” refers to alkynyl groups having two to six carbons.

As used herein, “cycloalkyl” refers to anon-aromatic carbocyclic ring,usually having from 3 to 8 ring carbon atoms. The ring may be saturatedor have one or more carbon-carbon double bonds. Examples of cycloalkylgroups include cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl,cyclohexyl, and cyclohexenyl, as well as bridged and caged ring groupssuch as norbornane.

As used herein, “alkoxy” refers to an alkyl group of the indicatednumber of carbon atoms attached through an oxygen bridge such as, forexample, methoxy, ethoxy, propoxy, isopropoxy, n-butoxy, sec-butoxy,tert-butoxy, pentyloxy, 2-pentyloxy, isopentyloxy, neopentyloxy,hexyloxy, 2-hexyloxy, 3-hexyloxy, 3-methylpentyloxy, and the like.Alkoxy groups will usually have from 1 to 7 carbon atoms attachedthrough the oxygen bridge. “Lower alkoxy” refers to alkoxy groups havingone to six carbons.

As used herein, “acyl” refers to the groups H—C(O)—; (alkyl)-C(O)—;(cycloalkyl)-C(O)—; (aryl)-C(O)—; (heteroaryl)-C(O)—; and(heterocycloalkyl)-C(O)—, wherein the group is attached to the parentstructure through the carbonyl functionality and wherein alkyl,cycloalkyl, aryl, heteroaryl, and heterocycloalkyl are as describedherein. Acyl groups have the indicated number of carbon atoms, with thecarbon of the keto group being included in the numbered carbon atoms.For example a C₂ acyl group is an acetyl group having the formulaCH₃(C═O)—.

As used herein, “formyl” refers to the group —C(O)H.

As used herein, “alkoxycarbonyl” refers to a group of the formula(alkoxy)(C═O)— attached through the carbonyl carbon wherein the alkoxygroup has the indicated number of carbon atoms. Thus a C₁-C₆alkoxycarbonyl group is an alkoxy group having from 1 to 6 carbon atomsattached through its oxygen to a carbonyl linker.

As used herein, “azido” refers to the group —N₃.

As used herein, “amino” refers to the group —NH₂.

As used herein, “mono- and di-(alkyl)amino” refers to secondary andtertiary alkyl amino groups, wherein the alkyl groups are as definedabove and have the indicated number of carbon atoms. The point ofattachment of the alkylamino group is on the nitrogen. Examples of mono-and di-alkylamino groups include ethylamino, dimethylamino, andmethyl-propyl-amino.

As used herein, “aminocarbonyl” refers to the group —CONR^(b)R^(c),where

R^(b) is chosen from H, optionally substituted C₁-C₆ alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl,optionally substituted alkoxy; and

R^(c) is chosen from hydrogen and optionally substituted C₁-C₄ alkyl; or

R^(b) and R^(c) taken together with the nitrogen to which they arebound, form an optionally substituted 5- to 8-memberednitrogen-containing heterocycloalkyl which optionally includes 1 or 2additional heteroatoms chosen from O, N, and S in the heterocycloalkylring;

where each substituted group is independently substituted with one ormore substituents independently chosen from C₁-C₄ alkyl, aryl,heteroaryl, aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl,—OC₁-C₄ alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄ haloalkyl,halo, —OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl),—NH(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄alkylphenyl), cyano, nitro, oxo (as a substituent for cycloalkyl,heterocycloalkyl, or heteroaryl), —CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄alkyl)(C₁-C₄ alkyl), —CONH(C₁-C₄ alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl),—NHC(O)(phenyl), —N(C₁-C₄ alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄alkyl)C(O)(phenyl), —C(O)C₁-C₄ alkyl, —C(O)C₁-C₄ alkylphenyl, —C(O)C₁-C₄haloalkyl, —OC(O)C₁-C₄ alkyl, —SO₂(C₁-C₄ alkyl), —SO₂(phenyl),—SO₂(C₁-C₄ haloalkyl), —SO₂NH₂, —SO₂NH(C₁-C₄ alkyl), —SO₂NH(phenyl),—NHSO₂(C₁-C₄ alkyl), —NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl).

As used herein, “aryl” refers to: 6-membered carbocyclic aromatic rings,for example, benzene; bicyclic ring systems wherein at least one ring iscarbocyclic and aromatic, for example, naphthalene, indane, andtetralin; and tricyclic ring systems wherein at least one ring iscarbocyclic and aromatic, for example, fluorene.

For example, aryl includes 6-membered carbocyclic aromatic rings fusedto a 5- to 7-membered heterocycloalkyl ring containing 1 or moreheteroatoms chosen from N, O, and S. For such fused, bicyclic ringsystems wherein only one of the rings is a carbocyclic aromatic ring,the point of attachment may be at the carbocyclic aromatic ring or theheterocycloalkyl ring. Bivalent radicals formed from substituted benzenederivatives and having the free valences at ring atoms are named assubstituted phenylene radicals. Bivalent radicals derived from univalentpolycyclic hydrocarbon radicals whose names end in “-yl” by removal ofone hydrogen atom from the carbon atom with the free valence are namedby adding “-idene” to the name of the corresponding univalent radical,e.g. a naphthyl group with two points of attachment is termednaphthylidene. Aryl, however, does not encompass or overlap in any waywith heteroaryl, separately defined below. Hence, if one or morecarbocyclic aromatic rings is fused with a heterocycloalkyl aromaticring, the resulting ring system is heteroaryl, not aryl, as definedherein.

As used herein, “aryloxy” refers to the group —O-aryl.

As used herein, “aralkyl” refers to the group -alkyl-aryl.

As used herein, “carbamimidoyl” refers to the group —C(═NH)—NH2.

As used herein, “substituted carbamimidoyl” refers to the group—C(═NR^(e))—NR^(f)R^(g) where

R^(e) is chosen from hydrogen, cyano, optionally substituted alkyl,optionally substituted cycloalkyl, optionally substituted aryl,optionally substituted heteroaryl, and optionally substitutedheterocycloalkyl; and

R^(f) and R^(g) are independently chosen from hydrogen optionallysubstituted alkyl, optionally substituted cycloalkyl, optionallysubstituted aryl, optionally substituted heteroaryl, and optionallysubstituted heterocycloalkyl,

provided that at least one of R^(e), R^(f), and R^(g) is not hydrogenand wherein substituted alkyl, cycloalkyl, aryl, heterocycloalkyl, andheteroaryl refer respectively to alkyl, cycloalkyl, aryl,heterocycloalkyl, and heteroaryl wherein one or more (such as up to 5,for example, up to 3) hydrogen atoms are replaced by a substituentindependently chosen from

—R^(a), —OR^(b), optionally substituted amino (including —NR^(c)COR^(b),—NR^(c)CO₂R^(a), —NR^(c)CONR^(b)R^(c), —NR^(b)C(NR^(c))NR^(b)R^(c),—NR^(b)C(NCN)NR^(b)R^(c), and —NR^(c)SO₂R^(a)), halo, cyano, nitro, oxo(as a substituent for cycloalkyl, heterocycloalkyl, and heteroaryl),optionally substituted acyl (such as —COR^(b)), optionally substitutedalkoxycarbonyl (such as —CO₂R^(b)), aminocarbonyl (such as—CONR^(b)R^(c)), —OCOR^(b), —OCO₂R^(a), —OCONR^(b)R^(c),—OP(O)(OR^(b))OR^(c), sulfanyl (such as SR^(b)), sulfinyl (such as—SOR^(a)), and sulfonyl (such as —SO₂R^(a) and —SO₂NR^(b)R^(c)),

where R^(a) is chosen from optionally substituted C1-C6 alkyl,optionally substituted aryl, and optionally substituted heteroaryl;

R^(b) is chosen from H, optionally substituted C1-C6 alkyl, optionallysubstituted aryl, and optionally substituted heteroaryl; and

R^(c) is chosen from hydrogen and optionally substituted C1-C4 alkyl; or

R^(b) and R^(c), and the nitrogen to which they are attached, form anoptionally substituted heterocycloalkyl group; and

where each optionally substituted group is unsubstituted orindependently substituted with one or more, such as one, two, or three,substituents independently chosen from C₁-C₄ alkyl, aryl, heteroaryl,aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl, —OC₁-C₄alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄haloalkyl, halo,—OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl), —NH(C₁-C₄alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄ alkylphenyl),cyano, nitro, oxo (as a substituent for cycloalkyl, heterocycloalkyl, orheteroaryl), —CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄ alkyl)(C₁-C₄ alkyl),—CONH(C₁-C₄ alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl), —NHC(O)(phenyl),—N(C₁-C₄ alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)C(O)(phenyl),—C(O)C1-C₄ alkyl, —C(O)C1-C₄ phenyl, —C(O)C₁-C₄ haloalkyl, —OC(O)C₁-C₄alkyl, —SO₂(C₁-C₄ alkyl), —SO₂(phenyl), —SO₂(C₁-C₄ haloalkyl), —SO₂NH₂,—SO₂NH(C₁-C₄ alkyl), —SO₂ NH(phenyl), —NHSO₂(C₁-C₄ alkyl),—NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl).

As used herein, “halo” refers to fluoro, chloro, bromo, and iodo, andthe term “halogen” includes fluorine, chlorine, bromine, and iodine.

As used herein, “haloalkyl” refers to alkyl as defined above having thespecified number of carbon atoms, substituted with 1 or more halogenatoms, up to the maximum allowable number of halogen atoms. Examples ofhaloalkyl include, but are not limited to, trifluoromethyl,difluoromethyl, 2-fluoroethyl, and penta-fluoroethyl.

As used herein, “heteroaryl” refers to:

5- to 7-membered aromatic, monocyclic rings containing one or more, forexample, from 1 to 4, or in certain embodiments, from 1 to 3,heteroatoms chosen from N, O, and S, with the remaining ring atoms beingcarbon;

bicyclic heterocycloalkyl rings containing one or more, for example,from 1 to 4, or in certain embodiments, from 1 to 3, heteroatoms chosenfrom N, O, and S, with the remaining ring atoms being carbon and whereinat least one heteroatom is present in an aromatic ring; and

tricyclic heterocycloalkyl rings containing one or more, for example,from 1 to 5, or in certain embodiments, from 1 to 4, heteroatoms chosenfrom N, O, and S, with the remaining ring atoms being carbon and whereinat least one heteroatom is present in an aromatic ring.

For example, heteroaryl includes a 5- to 7-membered heterocycloalkyl,aromatic ring fused to a 5- to 7-membered cycloalkyl or heterocycloalkylring. For such fused, bicyclic heteroaryl ring systems wherein only oneof the rings contains one or more heteroatoms, the point of attachmentmay be at either ring. When the total number of S and O atoms in theheteroaryl group exceeds 1, those heteroatoms are not adjacent to oneanother. In certain embodiments, the total number of S and O atoms inthe heteroaryl group is not more than 2. In certain embodiments, thetotal number of S and O atoms in the aromatic heterocycle is not morethan 1. Examples of heteroaryl groups include, but are not limited to,(as numbered from the linkage position assigned priority 1), 2-pyridyl,3-pyridyl, 4-pyridyl, 2,3-pyrazinyl, 3,4-pyrazinyl, 2,4-pyrimidinyl,3,5-pyrimidinyl, 2,3-pyrazolinyl, 2,4-imidazolyl, isoxazolyl, oxazolyl,thiazolyl, thiadiazolyl, tetrazolyl, thienyl, benzothiophenyl, furanyl,pyrrolyl, benzofuranyl, benzoimidazolyl, indolyl, pyridazinyl,triazolyl, quinolinyl, quinoxalinyl, pyrazolyl, and5,6,7,8-tetrahydroisoquinolinyl. Bivalent radicals derived fromunivalent heteroaryl radicals whose names end in “-yl” by removal of onehydrogen atom from the atom with the free valence are named by adding“-idene” to the name of the corresponding univalent radical, e.g. apyridyl group with two points of attachment is a pyridylidene.Heteroaryl does not encompass or overlap with aryl, cycloalkyl, orheterocycloalkyl, as defined herein

Substituted heteroaryl also includes ring systems substituted with oneor more oxide (—O—) substituents, such as pyridinyl N-oxides.

As used herein, “heterocycloalkyl” refers to a single, non-aromaticring, usually with 3 to 8 ring atoms, containing at least 2 carbon atomsin addition to 1-3 heteroatoms independently chosen from oxygen, sulfur,and nitrogen, as well as combinations comprising at least one of theforegoing heteroatoms. The ring may be saturated or have one or morecarbon-carbon double bonds. Suitable heterocycloalkyl groups include,for example (as numbered from the linkage position assigned priority 1),2-pyrrolidinyl, 2,4-imidazolidinyl, 2,3-pyrazolidinyl, 2-piperidyl,3-piperidyl, 4-piperidyl, 2,5-piperazinyl, pyrrolidinyl, azetidinyl,pyranyl, 2,3-dihydrofuranyl, or 2,5-dihydrofuranyl. Morpholinyl groupsare also contemplated, including 2-morpholinyl and 3-morpholinyl(numbered wherein the oxygen is assigned priority 1). Substitutedheterocycloalkyl also includes ring systems substituted with one or moreoxo (═O) or oxide (—O—) substituents, such as piperidinyl N-oxide,morpholinyl-N-oxide, 1-oxo-1-thiomorpholinyl and1,1-dioxo-1-thiomorpholinyl.

“Heterocycloalkyl” also includes bicyclic ring systems wherein onenon-aromatic ring, usually with 3 to 8 ring atoms, contains at least 2carbon atoms in addition to 1-3 heteroatoms independently chosen fromoxygen, sulfur, and nitrogen, as well as combinations comprising atleast one of the foregoing heteroatoms; and the other ring, usually with3 to 8 ring atoms, optionally contains 1-3 heteratoms independentlychosen from oxygen, sulfur, and nitrogen and is not aromatic.

As used herein, “sulfanyl” refers to the groups: —S-(optionallysubstituted (C₁-C₆)alkyl), —S-(optionally substituted aryl),—S-(optionally substituted heteroaryl), and —S-(optionally substitutedheterocycloalkyl). Hence, sulfanyl includes the group C₁-C₆alkylsulfanyl.

As used herein, “sulfinyl” refers to the groups: —S(O)-(optionallysubstituted (C₁-C₆)alkyl), —S(O)-optionally substituted aryl),—S(O)-optionally substituted heteroaryl), —S(O)-(optionally substitutedheterocycloalkyl); and —S(O)-(optionally substituted amino).

As used herein, “sulfonyl” refers to the groups: —S(O₂)-(optionallysubstituted (C₁-C₆)alkyl), —S(O₂)-optionally substituted aryl),—S(O₂)-optionally substituted heteroaryl), —S(O₂)-(optionallysubstituted heterocycloalkyl), and —S(O₂)-(optionally substitutedamino).

As used herein, “substituted” refers to any one or more hydrogens on thedesignated atom or group is replaced with a selection from the indicatedgroup, provided that the designated atom's normal valence is notexceeded. When a substituent is oxo (i.e. ═O) then 2 hydrogens on theatom are replaced. Combinations of substituents and/or variables arepermissible only if such combinations result in stable compounds oruseful synthetic intermediates. A stable compound or stable structure ismeant to imply a compound that is sufficiently robust to surviveisolation from a reaction mixture, and subsequent formulation as anagent having at least practical utility. Unless otherwise specified,substituents are named into the core structure. For example, it is to beunderstood that when (cycloalkyl)alkyl is listed as a possiblesubstituent, the point of attachment of this substituent to the corestructure is in the alkyl portion.

As used herein, the terms “substituted” alkyl, cycloalkyl, aryl,heterocycloalkyl, and heteroaryl, unless otherwise expressly defined,refer respectively to alkyl, cycloalkyl, aryl, heterocycloalkyl, andheteroaryl wherein one or more (such as up to 5, for example, up to 3)hydrogen atoms are replaced by a substituent independently chosen from

—R^(a), —OR^(b), optionally substituted amino (including —NR^(c)COR^(b),—NR^(c)CO₂R^(a), —NR^(c)CONR^(b)R^(c), —NR^(b)C(NR^(c))NR^(b)R^(c),—NR^(b)C(NCN)NR^(b)R^(c), and —NR^(c)SO₂R^(a)), halo, cyano, azido,nitro, oxo (as a substituent for cycloalkyl or heterocycloalkyl),optionally substituted acyl (such as —COR^(b)), optionally substitutedalkoxycarbonyl (such as —CO₂R^(b)), aminocarbonyl (such as—CONR^(b)R^(c)), —OCOR^(b), —OCO₂R^(a), —OCONR^(b)R^(c),—OP(O)(OR^(b))OR^(c), sulfanyl (such as SR^(b)), sulfinyl (such as—SOR^(a)), and sulfonyl (such as —SO₂R^(a) and —SO₂NR^(b)R^(c)), where

R^(a) is chosen from optionally substituted C₁-C₆ alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted alkenyl, optionally substituted alkynyl,optionally substituted aryl, and optionally substituted heteroaryl;R^(b) is chosen from hydrogen, optionally substituted C₁-C₆ alkyl,optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl; and

R^(c) is chosen from hydrogen and optionally substituted C₁-C₄ alkyl; or

R^(b) and R^(c), and the nitrogen to which they are attached, form anoptionally substituted heterocycloalkyl group; and

where each optionally substituted group is unsubstituted orindependently substituted with one or more, such as one, two, or three,substituents independently chosen from C1-C₄ alkyl, aryl, heteroaryl,aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl, —OC₁-C₄alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄haloalkyl, halo,—OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl), —NH(C₁-C₄alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄ alkylphenyl),cyano, nitro, oxo (as a substituent for cycloalkyl or heterocycloalkyl),—CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄ alkyl)(C₁-C₄ alkyl), —CONH(C₁-C₄alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl), —NHC(O)(phenyl), —N(C₁-C₄alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)C(O)(phenyl), —C(O)C₁-C₄ alkyl,—C(O)C₁-C₄ alkylphenyl, —C(O)C₁-C₄ haloalkyl, —OC(O)C₁-C₄ alkyl,—SO₂(C₁-C₄ alkyl), —SO₂(phenyl), —SO₂(C₁-C₄haloalkyl), —SO₂NH₂,—SO₂NH(C₁-C₄ alkyl), —SO₂NH(phenyl), —NHSO₂(C₁-C₄ alkyl),—NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl).

As used herein, “substituted acyl” refers to the groups (substitutedalkyl)-C(O)—; (substituted cycloalkyl)-C(O)—; (substituted aryl)-C(O)—;(substituted heteroaryl)-C(O)—; and (substitutedheterocycloalkyl)-C(O)—, wherein the group is attached to the parentstructure through the carbonyl functionality and wherein substitutedalkyl, cycloalkyl, aryl, heteroaryl, and heterocycloalkyl, referrespectively to alkyl, cycloalkyl, aryl, heteroaryl, andheterocycloalkyl wherein one or more (such as up to 5, for example, upto 3) hydrogen atoms are replaced by a substituent independently chosenfrom

—R^(a), —OR^(b), optionally substituted amino (including —NR^(c)COR^(b),—NR^(c)CO₂R^(a), —NR^(c)CONR^(b)R^(c), —NR^(b)C(NR^(c))NR^(b)R^(c),—NR^(b)C(NCN)NR^(b)R^(c), and —NR^(c)SO₂R^(a)), halo, cyano, nitro, oxo(as a substituent for cycloalkyl or heterocycloalkyl), optionallysubstituted acyl (such as —COR^(b)), optionally substitutedalkoxycarbonyl (such as —CO₂R^(b)), aminocarbonyl (such as—CONR^(b)R^(c)), —OCOR^(b), —OCO₂R^(a), —OCONR^(b)R^(c),—OP(O)(OR^(b))OR^(c), sulfanyl (such as SR^(b)), sulfinyl (such as—SOR^(a)), and sulfonyl (such as —SO₂R^(a) and —SO₂NR^(b)R^(c)),

where R^(a) is chosen from optionally substituted C₁-C₆ alkyl,optionally substituted alkenyl, optionally substituted alkynyl,optionally substituted aryl, and optionally substituted heteroaryl;

R^(b) is chosen from H, optionally substituted C₁-C₆ alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; and

R^(c) is chosen from hydrogen and optionally substituted C₁-C₄ alkyl; or

R^(b) and R^(c), and the nitrogen to which they are attached, form anoptionally substituted heterocycloalkyl group; and

where each optionally substituted group is unsubstituted orindependently substituted with one or more, such as one, two, or three,substituents independently chosen from C₁-C₄ alkyl, aryl, heteroaryl,aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl, —OC₁-C₄alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄haloalkyl, halo,—OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl), —NH(C₁-C₄alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄ alkylphenyl),cyano, nitro, oxo (as a substituent for cycloalkyl or heterocycloalkyl),—CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄ alkyl)(C₁-C₄ alkyl), —CONH(C₁-C₄alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl), —NHC(O)(phenyl), —N(C₁-C₄alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)C(O)(phenyl), —C(O)C₁-C₄ alkyl,—C(O)C₁-C₄ alkylphenyl, —C(O)C₁-C₄ haloalkyl, —OC(O)C₁-C₄ alkyl,—SO₂(C₁-C₄ alkyl), —SO₂(phenyl), —SO₂(C₁-C₄haloalkyl), —SO₂NH₂,—SO₂NH(C₁-C₄ alkyl), —SO₂NH(phenyl), —NHSO₂(C₁-C₄ alkyl),—NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl).

As used herein, “substituted alkoxy” refers to alkoxy wherein the alkylconstituent is substituted (i.e. —O-(substituted alkyl)) wherein“substituted alkyl” refers to alkyl wherein one or more (such as up to5, for example, up to 3) hydrogen atoms are replaced by a substituentindependently chosen from

—R^(a), —OR^(b), optionally substituted amino (including —NR^(c)COR^(b),—NR^(c)CO₂R^(a), —NR^(c)CONR^(b)R^(c), —NR^(b)C(NR^(c))NR^(b)R^(c),—NR^(b)C(NCN)NR^(b)R^(c), and —NR^(c)SO₂R^(a)), halo, cyano, nitro, oxo(as a substituent for cycloalkyl or heterocycloalkyl), optionallysubstituted acyl (such as —COR^(b)), optionally substitutedalkoxycarbonyl (such as —CO₂R^(b)), aminocarbonyl (such as—CONR^(b)R^(c)), —OCOR^(b), —OCO₂R^(a), —OCONR^(b)R^(c),—OP(O)(OR^(b))OR^(c), sulfanyl (such as SR^(b)), sulfinyl (such as—SOR^(a)), and sulfonyl (such as —SO₂R^(a) and —SO₂NR^(b)R^(c)),

where R^(a) is chosen from optionally substituted C₁-C₆ alkyl,optionally substituted alkenyl, optionally substituted alkynyl,optionally substituted aryl, and optionally substituted heteroaryl;

R^(b) is chosen from H, optionally substituted C₁-C₆ alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; and

R^(c) is chosen from hydrogen and optionally substituted C₁-C₄ alkyl; or

R^(b) and R^(c), and the nitrogen to which they are attached, form anoptionally substituted heterocycloalkyl group; and

where each optionally substituted group is unsubstituted orindependently substituted with one or more, such as one, two, or three,substituents independently chosen from C₁-C₄ alkyl, aryl, heteroaryl,aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl, —OC₁-C₄alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄haloalkyl, halo,—OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl), —NH(C₁-C₄alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄ alkylphenyl),cyano, nitro, oxo (as a substituent for cycloalkyl or heterocycloalkyl),—CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄ alkyl)(C₁-C₄ alkyl), —CONH(C₁-C₄alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl), —NHC(O)(phenyl), —N(C₁-C₄alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)C(O)(phenyl), —C(O)C₁-C₄ alkyl,—C(O)C₁-C₄ alkylphenyl, —C(O)C₁-C₄ haloalkyl, —OC(O)C₁-C₄ alkyl,—SO₂(C₁-C₄ alkyl), —SO₂(phenyl), —SO₂(C₁-C₄haloalkyl), —SO₂NH₂,—SO₂NH(C₁-C₄ alkyl), —SO₂NH(phenyl), —NHSO₂(C₁-C₄ alkyl),—NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl).

In some embodiments, a substituted alkoxy group is “polyalkoxy” or—O-(optionally substituted alkylene)-(optionally substituted alkoxy),and includes groups such as —OCH₂CH₂OCH₃, and residues of glycol etherssuch as polyethyleneglycol, and —O(CH₂CH₂O)_(x)CH₃, where x is aninteger of 2-20, such as 2-10, and for example, 2-5. Another substitutedalkoxy group is hydroxyalkoxy or —OCH₂(CH₂)_(y)OH, where y is an integerof 1-10, such as 1-4.

As used herein, “substituted alkoxycarbonyl” refers to the group(substituted alkyl)-O—C(O)— wherein the group is attached to the parentstructure through the carbonyl functionality and wherein substitutedrefers to alkyl wherein one or more (such as up to 5, for example, up to3) hydrogen atoms are replaced by a substituent independently chosenfrom

—R^(a), —OR^(b), optionally substituted amino (including —NR^(c)COR^(b),—NR^(c)CO₂R^(a), —NR^(c)CONR^(b)R^(c), —NR^(b)C(NR^(c))NR^(b)R^(c),—NR^(b)C(NCN)NR^(b)R^(c), and —NR^(c)SO₂R^(a)), halo, cyano, nitro, oxo(as a substituent for cycloalkyl or heterocycloalkyl), optionallysubstituted acyl (such as —COR^(b)), optionally substitutedalkoxycarbonyl (such as —CO₂R^(b)), aminocarbonyl (such as—CONR^(b)R^(c)), —OCOR^(b), —OCO₂R^(a), —OCONR^(b)R^(c),—OP(O)(OR^(b))OR^(c), sulfanyl (such as SR^(b)), sulfinyl (such as—SOR^(a)), and sulfonyl (such as —SO₂R^(a) and —SO₂NR^(b)R^(c)),

where R^(a) is chosen from optionally substituted C₁-C₆ alkyl,optionally substituted alkenyl, optionally substituted alkynyl,optionally substituted aryl, and optionally substituted heteroaryl;

R^(b) is chosen from H, optionally substituted C₁-C₆ alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; and

R^(c) is chosen from hydrogen and optionally substituted C₁-C₄ alkyl; or

R^(b) and R^(c), and the nitrogen to which they are attached, form anoptionally substituted heterocycloalkyl group; and

where each optionally substituted group is unsubstituted orindependently substituted with one or more, such as one, two, or three,substituents independently chosen from C₁-C₄ alkyl, aryl, heteroaryl,aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl, —OC₁-C₄alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄haloalkyl, halo,—OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl), —NH(C₁-C₄alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄ alkylphenyl),cyano, nitro, oxo (as a substituent for cycloalkyl or heterocycloalkyl),—CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄ alkyl)(C₁-C₄ alkyl), —CONH(C₁-C₄alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl), —NHC(O)(phenyl), —N(C₁-C₄alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)C(O)(phenyl), —C(O)C₁-C₄ alkyl,—C(O)C₁-C₄ alkylphenyl, —C(O)C₁-C₄ haloalkyl, —OC(O)C₁-C₄ alkyl,—SO₂(C₁-C₄ alkyl), —SO₂(phenyl), —SO₂(C₁-C₄haloalkyl), —SO₂NH₂,—SO₂NH(C₁-C₄ alkyl), —SO₂NH(phenyl), —NHSO₂(C₁-C₄ alkyl),—NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl).

As used herein, “substituted amino” refers to the group —NHR^(d) or—NR^(d)R^(e) wherein R^(d) is chosen from hydroxyl, formyl, optionallysubstituted alkoxy, optionally substituted alkyl, optionally substitutedcycloalkyl, optionally substituted acyl, optionally substitutedcarbamimidoyl, aminocarbonyl, optionally substituted aryl, optionallysubstituted heteroaryl, optionally substituted heterocycloalkyl,optionally substituted alkoxycarbonyl, sulfinyl and sulfonyl, andwherein R^(e) is chosen from optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted aryl, optionallysubstituted heteroaryl, and optionally substituted heterocycloalkyl, andwherein substituted alkyl, cycloalkyl, aryl, heterocycloalkyl, andheteroaryl refer respectively to alkyl, cycloalkyl, aryl,heterocycloalkyl, and heteroaryl wherein one or more (such as up to 5,for example, up to 3) hydrogen atoms are replaced by a substituentindependently chosen from

—R^(a), —OR^(b), optionally substituted amino (including —NR^(c)COR^(b),—NR^(c)CO₂R^(a), —NR^(c)CONR^(b)R^(c), —NR^(b)C(NR^(c))NR^(b)R^(c),—NR^(b)C(NCN)NR^(b)R^(c), and —NR^(c)SO₂R^(a)), halo, cyano, nitro, oxo(as a substituent for cycloalkyl or heterocycloalkyl), optionallysubstituted acyl (such as —COR^(b)), optionally substitutedalkoxycarbonyl (such as —CO₂R^(b)), aminocarbonyl (such as—CONR^(b)R^(c)), —OCOR^(b), —OCO₂R^(a), —OCONR^(b)R^(c),—OP(O)(OR^(b))OR^(c), sulfanyl (such as SR^(b)), sulfinyl (such as—SOR^(a)), and sulfonyl (such as —SO₂R^(a) and —SO₂NR^(b)R^(c)),

where R^(a) is chosen from optionally substituted C₁-C₆ alkyl,optionally substituted alkenyl, optionally substituted alkynyl,optionally substituted aryl, and optionally substituted heteroaryl;

R^(b) is chosen from H, optionally substituted C₁-C₆ alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; and

R^(c) is chosen from hydrogen and optionally substituted C₁-C₄ alkyl; or

R^(b) and R^(c), and the nitrogen to which they are attached, form anoptionally substituted heterocycloalkyl group; and

where each optionally substituted group is unsubstituted orindependently substituted with one or more, such as one, two, or three,substituents independently chosen from C₁-C₄ alkyl, aryl, heteroaryl,aryl-C₁-C₄ alkyl-, heteroaryl-C₁-C₄ alkyl-, C₁-C₄ haloalkyl, —OC₁-C₄alkyl, —OC₁-C₄ alkylphenyl, —C₁-C₄ alkyl-OH, —OC₁-C₄haloalkyl, halo,—OH, —NH₂, —C₁-C₄ alkyl-NH₂, —N(C₁-C₄ alkyl)(C₁-C₄ alkyl), —NH(C₁-C₄alkyl), —N(C₁-C₄ alkyl)(C₁-C₄ alkylphenyl), —NH(C₁-C₄ alkylphenyl),cyano, nitro, oxo (as a substituent for cycloalkyl or heterocycloalkyl),—CO₂H, —C(O)OC₁-C₄ alkyl, —CON(C₁-C₄ alkyl)(C₁-C₄ alkyl), —CONH(C₁-C₄alkyl), —CONH₂, —NHC(O)(C₁-C₄ alkyl), —NHC(O)(phenyl), —N(C₁-C₄alkyl)C(O)(C₁-C₄ alkyl), —N(C₁-C₄ alkyl)C(O)(phenyl), —C(O)C₁-C₄ alkyl,—C(O)C₁-C₄ alkylphenyl, —C(O)C₁-C₄ haloalkyl, —OC(O)C₁-C₄ alkyl,—SO₂(C₁-C₄ alkyl), —SO₂(phenyl), —SO₂(C₁-C₄haloalkyl), —SO₂NH₂,—SO₂NH(C₁-C₄ alkyl), —SO₂NH(phenyl), —NHSO₂(C₁-C₄ alkyl),—NHSO₂(phenyl), and —NHSO₂(C₁-C₄ haloalkyl); and

wherein optionally substituted acyl, optionally substitutedalkoxycarbonyl, sulfinyl and sulfonyl are as defined herein.

The term “substituted amino” also refers to N-oxides of the groups—NHR^(d), and NR^(d)R^(d) each as described above. N-oxides can beprepared by treatment of the corresponding amino group with, forexample, hydrogen peroxide or m-chloroperoxybenzoic acid. The personskilled in the art is familiar with reaction conditions for carrying outthe N-oxidation.

Compounds described herein include, but are not limited to, theiroptical isomers, racemates, and other mixtures thereof. In thosesituations, the single enantiomers or diastereomers, i.e., opticallyactive forms, can be obtained by asymmetric synthesis or by resolutionof the racemates. Resolution of the racemates can be accomplished, forexample, by conventional methods such as crystallization in the presenceof a resolving agent, or chromatography, using, for example a chiralhigh-pressure liquid chromatography (HPLC) column. In addition,compounds include Z- and E-forms (or cis- and trans-forms) of compoundswith carbon-carbon double bonds. Where compounds described herein existin various tautomeric forms, the term “compound” is intended to includeall tautomeric forms of the compound.

Compounds of Formula I also include crystalline and amorphous forms ofthose compounds, including, for example, polymorphs, pseudopolymorphs,solvates (including hydrates), unsolvated polymorphs (includinganhydrates), conformational polymorphs, and amorphous forms of thecompounds, as well as mixtures thereof. “Crystalline form,” “polymorph,”and “novel form” may be used interchangeably herein, and are meant toinclude all crystalline and amorphous forms of the compound, including,for example, polymorphs, pseudopolymorphs, solvates (includinghydrates), unsolvated polymorphs (including anhydrates), conformationalpolymorphs, and amorphous forms, as well as mixtures thereof, unless aparticular crystalline or amorphous form is referred to. Similarly,“pharmaceutically acceptable salts of compounds of Formula I alsoinclude crystalline and amorphous forms of those compounds, including,for example, polymorphs, pseudopolymorphs, solvates (includinghydrates), unsolvated polymorphs (including anhydrates), conformationalpolymorphs, and amorphous forms of the pharmaceutically acceptablesalts, as well as mixtures thereof.

A “solvate” is formed by the interaction of a solvent and a compound.The term “compound” is intended to include solvates of compounds.Similarly, “pharmaceutically acceptable salts” includes solvates ofpharmaceutically acceptable salts. Suitable solvates arepharmaceutically acceptable solvates, such as hydrates, includingmonohydrates and hemi-hydrates.

Compounds of Formula I also include other pharmaceutically acceptableforms of the recited compounds, including chelates, non-covalentcomplexes, prodrugs, and mixtures thereof.

A “chelate” is formed by the coordination of a compound to a metal ionat two (or more) points. The term “compound” is intended to includechelates of compounds. Similarly, “pharmaceutically acceptable salts”includes chelates of pharmaceutically acceptable salts.

A “non-covalent complex” is formed by the interaction of a compound andanother molecule wherein a covalent bond is not formed between thecompound and the molecule. For example, complexation can occur throughvan der Waals interactions, hydrogen bonding, and electrostaticinteractions (also called ionic bonding). Such non-covalent complexesare included in the term “compound”. Similarly, “pharmaceuticallyacceptable salts” includes “non-covalent complexes” of pharmaceuticallyacceptable salts.

The term “hydrogen bond” refers to a form of association between anelectronegative atom (also known as a hydrogen bond acceptor) and ahydrogen atom attached to a second, relatively electronegative atom(also known as a hydrogen bond donor). Suitable hydrogen bond donor andacceptors are well understood in medicinal chemistry.

“Hydrogen bond acceptor” refers to a group comprising an oxygen ornitrogen, such as an oxygen or nitrogen that is sp²-hybridized, an etheroxygen, or the oxygen of a sulfoxide or N-oxide.

The term “hydrogen bond donor” refers to an oxygen, nitrogen, orheteroaromatic carbon that bears a hydrogen.group containing a ringnitrogen or a heteroaryl group containing a ring nitrogen.

The compounds disclosed herein can be used in different enrichedisotopic forms, e.g., enriched in the content of ²H, ³H, ¹¹C, ¹³C and/or¹⁴C. In one particular embodiment, the compound is deuterated at atleast one position. Such deuterated forms can be made by the proceduredescribed in U.S. Pat. Nos. 5,846,514 and 6,334,997. As described inU.S. Pat. Nos. 5,846,514 and 6,334,997, deuteration can improve theefficacy and increase the duration of action of drugs.

Deuterium substituted compounds can be synthesized using various methodssuch as described in: Dean, Dennis C.; Editor. Recent Advances in theSynthesis and Applications of Radiolabeled Compounds for Drug Discoveryand Development. [In: Curr., Pharm. Des., 2000; 6(10)] 2000, 110 pp;George W.; Varma, Rajender S. The Synthesis of Radiolabeled Compoundsvia Organometallic Intermediates, Tetrahedron, 1989, 45(21), 6601-21;and Evans, E. Anthony. Synthesis of radiolabeled compounds, J.Radioanal. Chem., 1981, 64(1-2), 9-32.

“Pharmaceutically acceptable salts” include, but are not limited tosalts with inorganic acids, such as hydrochlorate, phosphate,diphosphate, hydrobromate, sulfate, sulfinate, nitrate, and like salts;as well as salts with an organic acid, such as malate, maleate,fumarate, tartrate, succinate, citrate, acetate, lactate,methanesulfonate, p-toluenesulfonate, 2-hydroxyethylsulfonate, benzoate,salicylate, stearate, and alkanoate such as acetate, HOOC—(CH₂)_(n)—COOHwhere n is 0-4, and like salts. Similarly, pharmaceutically acceptablecations include, but are not limited to sodium, potassium, calcium,aluminum, lithium, and ammonium.

In addition, if the compounds described herein are obtained as an acidaddition salt, the free base can be obtained by basifying a solution ofthe acid salt. Conversely, if the product is a free base, an additionsalt, particularly a pharmaceutically acceptable addition salt, may beproduced by dissolving the free base in a suitable organic solvent andtreating the solution with an acid, in accordance with conventionalprocedures for preparing acid addition salts from base compounds. Thoseskilled in the art will recognize various synthetic methodologies thatmay be used to prepare non-toxic pharmaceutically acceptable additionsalts.

“Prodrugs” described herein include any compound that becomes a compoundof Formula I when administered to a subject, e.g., upon metabolicprocessing of the prodrug. Similarly, “pharmaceutically acceptablesalts” includes “prodrugs” of pharmaceutically acceptable salts.Examples of prodrugs include derivatives of functional groups, such as acarboxylic acid group, in the compounds of Formula I. Exemplary prodrugsof a carboxylic acid group include, but are not limited to, carboxylicacid esters such as alkyl esters, hydroxyalkyl esters, arylalkyl esters,and aryloxyalkyl esters. Other exemplary prodrugs include lower alkylesters such as ethyl ester, acyloxyalkyl esters such aspivaloyloxymethyl (POM), glycosides, and ascorbic acid derivatives.

Other exemplary prodrugs include amides of carboxylic acids. Exemplaryamide prodrugs include metabolically labile amides that are formed, forexample, with an amine and a carboxylic acid. Exemplary amines includeNH₂, primary, and secondary amines such as NHR^(x), and NR^(x)R^(y),wherein R^(x) is hydrogen, (C₁-C₁₈)-alkyl, (C₃-C₇)-cycloalkyl,(C₃-C₇)-cycloalkyl-(C₁-C₄)-alkyl-, (C₆-C₁₄)-aryl which is unsubstitutedor substituted by a residue (C₁-C₂)-alkyl, (C₁-C₂)-alkoxy, fluoro, orchloro; heteroaryl-, (C₆-C₁₄)-aryl-(C₁-C₄)-alkyl- where aryl isunsubstituted or substituted by a residue (C₁-C₂)-alkyl, (C₁-C₂)-alkoxy,fluoro, or chloro; or heteroaryl-(C₁-C₄)-alkyl- and in which R^(y) hasthe meanings indicated for R^(x) with the exception of hydrogen orwherein R^(x) and R^(y), together with the nitrogen to which they arebound, form an optionally substituted 4- to 8-membered heterocycloalkylring which optionally includes one or two additional heteroatoms chosenfrom nitrogen, oxygen, and sulfur. A discussion of prodrugs is providedin T. Higuchi and V. Stella, Pro-drugs as Novel Delivery Systems, Vol.14 of the A.C.S. Symposium Series, in Edward B. Roche, ed.,Bioreversible Carriers in Drug Design, American PharmaceuticalAssociation and Pergamon Press, 1987, and in Design of Prodrugs, ed. H.Bundgaard, Elsevier, 1985.

As used herein the terms “group”, “radical” or “fragment” are synonymousand are intended to indicate functional groups or fragments of moleculesattachable to a bond or other fragments of molecules.

As used herein, “modulation” refers to a change in activity as a director indirect response to the presence of a chemical entity as describedherein, relative to the activity of in the absence of the chemicalentity. The change may be an increase in activity or a decrease inactivity, and may be due to the direct interaction of the compound withthe a target or due to the interaction of the compound with one or moreother factors that in turn affect the target's activity. For example,the presence of the chemical entity may, for example, increase ordecrease the target activity by directly binding to the target, bycausing (directly or indirectly) another factor to increase or decreasethe target activity, or by (directly or indirectly) increasing ordecreasing the amount of target present in the cell or organism.

As used herein, “active agent” is used to indicate a chemical entitywhich has biological activity. In certain embodiments, an “active agent”is a compound having pharmaceutical utility. For example an active agentmay be an anti-cancer therapeutic.

As used herein, “significant” refers to any detectable change that isstatistically significant in a standard parametric test of statisticalsignificance such as Student's T-test, where p<0.05.

As used herein, a “pharmaceutically acceptable” component is one that issuitable for use with humans and/or animals without undue adverse sideeffects (such as toxicity, irritation, and allergic response)commensurate with a reasonable benefit/risk ratio.

As used herein, “therapeutically effective amount” of a chemical entitydescribed herein refers to an amount effective, when administered to ahuman or non-human subject, to provide a therapeutic benefit such asamelioration of symptoms, slowing of disease progression, or preventionof disease.

“Treating” or “treatment” encompasses administration of at least onecompound of Formula I, or a pharmaceutically acceptable salt thereof, toa mammalian subject, particularly a human subject, in need of such anadministration and includes (i) arresting the development of clinicalsymptoms of the disease, such as cancer, (ii) bringing about aregression in the clinical symptoms of the disease, such as cancer,and/or (iii) prophylactic treatment for preventing the onset of thedisease, such as cancer.

As used herein, “cancer” refers to all types of cancer or neoplasm ormalignant tumors found in mammals, including carcinomas and sarcomas.Examples of cancer are cancer of the brain, breast, cervix, colon, head& neck, kidney, lung, non-small cell lung, melanoma, mesothelioma,ovary, sarcoma, stomach, uterus and Medulloblastoma.

As used herein, “subject” refers to a mammal that has been or will bethe object of treatment, observation or experiment. The methodsdescribed herein can be useful in both human therapy and veterinaryapplications. In some embodiments, the subject is a human.

The term “mammal” is intended to have its standard meaning, andencompasses humans, dogs, cats, sheep, and cows, for example.

Provided is at least one chemical entity chosen from compounds ofFormula I

and pharmaceutically acceptable salts thereof, wherein

R₁, R₂, R₃, R₄, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independently chosenfrom hydrogen, hydroxy, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, optionallysubstituted alkynyl, optionally substituted alkoxy, optionallysubstituted aryloxy, optionally substituted heteroaryloxy, optionallysubstituted heterocycloalkyloxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino; or

R₁ and R₂, or R₅ and R₆, or R₇ and R₈, or R₉ and R₁₀, or R₁ and R₁₂mutually independently, together in each case denote an oxo group (═O);or

R₄ and R₅ may optionally be joined together with any intervening atomsto form an optionally substituted heterocycloalkyl ring;

R₇ is chosen from hydrogen, hydroxy, optionally substituted alkoxy,optionally substituted aryloxy, optionally substituted heteroaryloxy,optionally substituted heterocycloalkyloxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino;

R₈ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, and optionallysubstituted alkynyl;

R₁₃ is chosen from hydrogen, optionally substituted alkyl, and formyl;

R₁₄ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl; and

R₁₅ is chosen from hydrogen, hydroxyl, formyl, optionally substitutedalkoxy, optionally substituted alkyl, optionally substituted cycloalkyl,optionally substituted heterocycloalkyl, optionally substituted aryl,and optionally substituted heteroaryl, —COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈,—C(NR₁₉)NR₁₇R₁₈, —C(NCN)NR₁₇R₁₈, —SO₂R₁₆, and —SO₂NR₁₇R₁₈, where R₁₆ ischosen from optionally substituted alkyl, optionally substitutedcycloalkyl, optionally substituted heterocycloalkyl, optionallysubstituted aryl, and optionally substituted heteroaryl; and R₁₇, R₁₈and R₁₉ are independently chosen from hydrogen, optionally substitutedalkyl, optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl; or R₁₇ and R₁₈ may be joined together with anyintervening atoms to form an optionally substituted heterocycloalkylring, or

R₁₄ and R₁₅ are joined together with any intervening atoms to form anoptionally substituted 4- to 8-membered heterocycloalkyl or optionallysubstituted 5- to 8-membered heteroaryl ring;

W₁ is chosen from the following moieties:

wherein Y is chosen from O and NR₂₁;

R₂₀ is chosen from cyano, halo, hydroxy, azido, nitro, carboxy,sulfinyl, sulfanyl, optionally substituted alkoxy, optionallysubstituted aryloxy, optionally substituted heteroaryloxy, optionallysubstituted heterocycloalkyloxy, optionally substituted alkoxycarbonyl,optionally substituted alkyl, optionally substituted alkenyl, optionallysubstituted aryloxy, optionally substituted aryl, optionally substitutedheteroaryl, optionally substituted heterocycloalkyl, optionallysubstituted amino, optionally substituted acyl, optionally substitutedalkoxycarbonyl, optionally substituted aminocarbonyl, optionallysubstituted aminosulfonyl, optionally substituted carbaminodoyl, andoptionally substituted alkynyl;

R₂₁ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted heterocycloalkyl,optionally substituted aryl, and optionally substituted heteroaryl;

W₂ is chosen from hydrogen, optionally substituted alkyl, optionallysubstituted cycloalkyl, optionally substituted alkenyl, and optionallysubstituted alkynyl;

m is selected from 0, 1, 2, and 3;

n, p, and q is independently selected from 0 and 1; and

the dotted line represents a single bond or a double bond.

In some embodiments, R₁₅ is —COR₁₆ and R₁₆ is not methyl, ethyl,cyclopentyl, or phenyl.

In other embodiments, R₁₄ is hydrogen, R₁₅ is —CONR₁₇R₁₈, and R₁₇ andR₁₈ taken together form a ring which is not a piperidine, piperazine,morpholine, or diazepane ring.

In other embodiments, R₁₄ is hydrogen, R₁₅ is —CONR₁₇R₁₈, and R₁₇ or R₁₈are not ethyl, aminoethyl, piperidinyl, or piperidinylmethyl.

In some embodiments, the compound of Formula I is not

In some embodiments, R₁, R₂, R₃, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ areindependently chosen from hydrogen, hydroxy, optionally substitutedalkyl, optionally substituted alkoxy, optionally substitutedaminocarbonyloxy, optionally substituted acyloxy, optionally substitutedalkoxycarbonyloxy, and optionally substituted amino. In someembodiments, R₁, R₂, R₃, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independentlychosen from hydrogen, hydroxy, and optionally substituted alkyl. In someembodiments, R₁, R₂, R₃, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independentlychosen from hydrogen, hydroxy, and lower alkyl. In some embodiments, R₁,R₂, R₃, R₅, R₆, R₉, R₁₀, R₁₁ and R₁₂ are independently chosen fromhydrogen, hydroxy, and methyl. In some embodiments, R₁, R₂, R₅, R₆, R₉,R₁₀, R₁₁ and R₁₂ are independently chosen from hydrogen, hydroxy, andmethyl; R₃ is chosen from hydroxyl and hydrogen. In some embodiments, atleast one of R₁ and R₂, or R₅ and R₆, or R₇ and R₈, or R₉ and R₁₀, orR₁₁ and R₁₂ mutually independently, together in each case denotes an oxogroup (═O).

In some embodiments, R₄ is hydroxy,

In some embodiments, R₄ and R₅ are joined together with any interveningatoms to form an optionally substituted 3- to 8-memberedheterocycloalkyl ring. In some embodiments, R₄ and R₅ are joinedtogether with any intervening atoms to form an oxirane ring.

In some embodiments, R₇ is chosen from hydrogen, hydroxy, optionallysubstituted alkoxy, optionally substituted aminocarbonyloxy, optionallysubstituted acyloxy, optionally substituted alkoxycarbonyloxy, andoptionally substituted amino. In some embodiments, R₇ is chosen fromhydrogen and optionally substituted acyloxy. In some embodiments, R₇ ischosen from hydrogen and acyloxy. In some embodiments, R₇ is chosen fromhydrogen and —OCOCH₃.

In some embodiments, R₈ and W₂ are independently chosen from hydrogenand optionally substituted alkyl. In some embodiments, R₈ and W₂ areindependently chosen from hydrogen and lower alkyl. In some embodiments,R₈ is hydrogen. In some embodiments, W₂ is hydrogen.

In some embodiments, R₁₃ is chosen from hydrogen and optionallysubstituted alkyl. In some embodiments, R₁₃ is chosen from hydrogen andloweralkyl. In some embodiments, R₁₃ is chosen from hydrogen, methyl,and hydroxymethyl.

In some embodiments, R₁₄ is chosen from hydrogen, optionally substitutedlower alkyl, optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl. In some embodiments, R₁₄ is chosen from hydrogenand optionally substituted lower alkyl. In some embodiments, R₁₄ ishydrogen.

In some embodiments, R₁₅ is chosen from hydrogen, optionally substitutedalkyl, optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, —COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈, —C(NR₁₉)NR₁₇R₁₈,—C(NCN)NR₁₇R₁₈, —SO₂R₁₆, and —SO₂NR₁₇R₁₈.

In some embodiments, R₁₅ is lower alkyl optionally substituted withhydroxyl, optionally substituted amino, or optionally substitutedheterocycloalkyl. In some embodiments, R₁₅ is lower alkyl optionallysubstituted with hydroxyl, optionally substituted amino, or pyrrolidineoptionally substituted with oxo.

In some embodiments, R₁₅ is chosen from —COR₁₆, —CO₂R₁₆, —CONR₁₇R₁₈, and—SO₂NR₁₇R₁₈. In some embodiments, R₁₅ is chosen from —COR₁₆, —CO₂R₁₆,and —CONR₁₇R₁₈.

In some embodiments, R₁₅ is —CONR₁₇R₁₈ and R₁₄ taken together with R₁₇form a 5- or 6-membered, optionally substituted, heterocyclic ring.

In some embodiments, R₁₆ is chosen from optionally substituted alkyl,optionally substituted cycloalkyl, optionally substitutedheterocycloalkyl, optionally substituted aryl, and optionallysubstituted heteroaryl. In some embodiments, R₁₆ is chosen fromoptionally substituted alkyl, optionally substituted cycloalkyl, andoptionally substituted heterocycloalkyl. In some embodiments, R₁₆ ischosen from alkyl optionally substituted with one or two groupsindependently hydroxyl, optionally substituted amino, lower alkoxy, andheterocycloalkyl, wherein heterocycloalkyl is optionally substitutedwith oxo. In some embodiments, R₁₆ is methyl, lower alkyl substitutedwith heterocycloalkyl, lower alkyl substituted with optionallysubstituted amino, or heterocycloalkyl. In some embodiments, R₁₆ ismethyl, lower alkyl substituted with heterocycloalkyl, lower alkylsubstituted with amino, or heterocycloalkyl.

In some embodiments, R₁₇ and R₁₈ are independently chosen from hydrogen,optionally substituted alkyl, optionally substituted cycloalkyl,optionally substituted heterocycloalkyl, optionally substituted aryl,and optionally substituted heteroaryl. In some embodiments, R₁₇ and R₁₈are independently chosen from hydrogen, optionally substituted alkyl,optionally substituted cycloalkyl, and optionally substitutedheterocycloalkyl. In some embodiments, R₁₇ is hydrogen. In someembodiments, R₁₈ is lower alkyl optionally substituted with optionallysubstituted amino or hydroxyl.

In some embodiments, R₁₇ and R₁₈ are joined together with anyintervening atoms to form an optionally substituted 4- to 8-memberedheterocycloalkyl ring.

In some embodiments, R₁₇ and R₁₈ are joined together to form a 4- to8-membered heterocycloalkyl ring optionally substituted with one or twogroups independently chosen from amino, hydroxyl, oxo, and lower alkyl.

In some embodiments, R₁₇ and R₁₈ are joined together to form a 5- to7-membered heterocycloalkyl ring chosen from morpholinyl, piperazinyl,diazepanyl, piperidinyl, or pyrrolidinyl.

In some embodiments, R₁₇ and R₁₈ are joined together to form a 5- to7-membered heterocycloalkyl ring chosen from 3-hydroxypyrrolidine-1-yl,3-aminopyrrolidine-1-yl, 3-oxopiperazine-1-yl,4-methyl-1,4-diazepane-1-yl, 1,4-diazepane-1-yl, piperazine-1-yl,4-methylpiperazine-1-yl, and morpholine-4-yl.

In some embodiments, R₁₉ is chosen from hydrogen, optionally substitutedalkyl, optionally substituted cycloalkyl, and optionally substitutedheterocycloalkyl. In some embodiments, R₁₉ is chosen from hydrogen andoptionally substituted alkyl.

In some embodiments, R₁₄ and R₁₅ are joined together with anyintervening atoms to form an optionally substituted 4- to 8-memberedheterocycloalkyl or optionally substituted 5- to 8-membered heteroarylring.

In some embodiments, R₁₄ and R₁₅ are joined together with anyintervening atoms to form an optionally substituted 4- to 8-memberedheterocycloalkyl ring. In some embodiments, R₁₄ and R₁₅ are joinedtogether with any intervening atoms to form an morpholin-4-yl,piperidin-1-yl, piperidin-4-yl, piperazin-1-yl, pyrrolidin-1-yl,pyrrolidin-2-yl, each of which is optionally substituted.

In some embodiments, R₁₄ and R₁₅ are joined together with anyintervening atoms to form an optionally substituted 5- to 8-memberedheteroaryl ring. In some embodiments, R₁₄ and R₁₅ are joined togetherwith any intervening atoms to form imidazolyl, or pyrazolyl, each ofwhich is optionally substituted.

In some embodiments, Y is chosen from O, NH and NCH₃. In someembodiments, Y is O.

In some embodiments, R₂₀ is chosen from cyano, halo, hydroxy, carboxy,sufonyl, optionally substituted alkoxy, optionally substitutedalkoxycarbonyl, optionally substituted alkyl, optionally substitutedamino, optionally substituted acyl, optionally substitutedalkoxycarbonyl, optionally substituted aminocarbonyl, and optionallysubstituted aminosulfonyl.

In some embodiments, m is 0.

In some embodiments, the dotted line represents a single bond.

In some embodiments, the dotted line represents a double bond.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ia.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ib.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ic.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Id.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ie.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula If.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ig.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ih.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ii.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ij.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Ik.

Also provided is at least one chemical entity of claim 1 wherein thecompound of Formula I is chosen from compounds of Formula Il.

Also provided is at least one chemical entity chosen from

-   2-aminoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-hydroxyethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-((R)-3-hydroxypyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-(2-aminoethyl)-3-((3S,5S,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methylpiperazine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(4-methylpiperazin-1-yl)ethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid,-   N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-oxopiperazine-1-carboxamide,-   (S)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   (R)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-morpholinoacetamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (S)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(((2-morpholinoethoxy)carbonyl)amino)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(((2-(3-oxopiperazin-1-yl)ethoxy)carbonyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(3-(2-(pyrrolidin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(3-(2-morpholinoethyl)ureido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methylpiperazine-1-carboxamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(3-(2-(4-methylpiperazin-1-yl)ethyl)ureido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(morpholine-4-carboxamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   4-(3-((3S,5R,8R,9S,10S,13R,14S,16S,17R)-16-acetoxy-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(piperazine-1-carboxamido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3-(1,4-diazepane-1-carboxamido)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methyl-1,4-diazepane-1-carboxamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(3-oxopiperazine-1-carboxamido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(3-(2-(2-oxopiperazin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)ureido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(3-(2-(3-oxopiperazin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   2-aminoethyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-(2-aminoethyl)-3-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(piperazin-1-yl)ethyl)urea,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methylpiperazine-1-carboxamide,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-oxopiperazine-1-carboxamide,-   (S)—N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxypyrrolidine-1-carboxamide,-   (R)—N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxypyrrolidine-1-carboxamide,-   (S)-3-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   (R)-3-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   2-(pyrrolidin-1-yl)ethyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(piperazin-1-yl)ethyl)urea,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methylpiperazine-1-carboxamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-oxopiperazine-1-carboxamide,-   (S)-3-hydroxy-N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   (R)-3-hydroxy-N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   2-(pyrrolidin-1-yl)ethyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)carbamate,-   2-morpholinoethyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)carbamate,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-3-methylurea,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-3-(2-morpholinoethyl)urea,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-4-methylpiperazine-1-carboxamide,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-3-(2-(4-methylpiperazin-1-yl)ethyl)urea,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((1R,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)morpholine-4-carboxamide,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(((2-morpholinoethoxy)carbonyl)amino)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(((2-(3-oxopiperazin-1-yl)ethoxy)carbonyl)amino)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-(2-(pyrrolidin-1-yl)ethyl)ureido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(3-(2-morpholinoethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(4-methylpiperazine-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(3-(2-(4-methylpiperazin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(morpholine-4-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(4-methyl-1,4-diazepane-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-oxopiperazine-1-carboxamido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-(2-(3-oxopiperazin-1-yl)ethyl)ureido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(((2-morpholinoethoxy)carbonyl)amino)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(((2-(3-oxopiperazin-1-yl)ethoxy)carbonyl)amino)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-(2-(pyrrolidin-1-yl)ethyl)ureido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(3-(2-morpholinoethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(4-methylpiperazine-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(3-(2-(4-methylpiperazin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(morpholine-4-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(4-methyl-1,4-diazepane-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-oxopiperazine-1-carboxamido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-(2-(3-oxopiperazin-1-yl)ethyl)ureido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   2-aminoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-hydroxyethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(piperazin-1-yl)ethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-oxopiperazine-1-carboxamide,-   (S)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   (R)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (S)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(piperazin-1-yl)ethyl)urea,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide-   4-(3-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxypyrrolidine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxypyrrolidine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(((2-morpholinoethoxy)carbonyl)amino)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(((2-(3-oxopiperazin-1-yl)ethoxy)carbonyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(3-(2-(pyrrolidin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(3-(2-morpholinoethyl)ureido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(piperazine-1-carboxamido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(3-(2-(piperazin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(morpholine-4-carboxamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   4-(3-((3S,5R,8R,9S,10S,13R,14S,16S,17R)-16-acetoxy-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methylpiperazine-1-carboxamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3-(1,4-diazepane-1-carboxamido)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methyl-1,4-diazepane-1-carboxamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(3-(2-(2-oxopiperazin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(3-(2-(3-oxopiperazin-1-yl)ethyl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid-   N-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-morpholinoacetamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)-2-amino-N1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (S)-2-amino-N1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-morpholinoethyl)urea,-   N-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)piperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)piperazine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(piperazin-1-yl)ethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)ureido)butanoic    acid,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxypyrrolidine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxypyrrolidine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)urea,-   2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,-   (2R)-2-amino-N-((3S,5R,8R,9S,10S,13S,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)-2-amino-N1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (S)-2-amino-N1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-3-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-3-carboxamide,-   5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   1-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea,-   1-(2-aminoethyl)-3-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylmorpholine-4-carboxamide,-   methyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   methyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,-   (R)-2-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)—N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (R)—N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   4-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one,-   5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   methyl    ((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   (2R)-2-amino-N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylmorpholine-4-carboxamide,-   5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   (2R)-2-amino-N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   (2R)—N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((1-methylpiperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3R)-3-fluoropiperidin-4-yl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3S)-3-fluoropiperidin-4-yl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3R)-3-fluoropiperidin-4-yl)(methyl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3S)-3-fluoropiperidin-4-yl)(methyl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3R)-3-fluoro-1-methylpiperidin-4-yl)(methyl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3S)-3-fluoro-1-methylpiperidin-4-yl)(methyl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3R)-3-fluoro-1-methylpiperidin-4-yl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(((3S)-3-fluoro-1-methylpiperidin-4-yl)amino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperidin-4-ylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl(1-methylpiperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl(piperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(4-aminopiperidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(4-hydroxypiperidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(3-hydroxypiperidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(3-aminopiperidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-3-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-3-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-3-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-3-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-2-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-2-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-2-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-2-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-2-(hydroxymethyl)pyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-2-(aminomethyl)pyrrolidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-2-(aminomethyl)pyrrolidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-3-aminopyrrolidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-3-aminopyrrolidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-(1,4-diazepan-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methyl-1,4-diazepan-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(1H-imidazol-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(1H-pyrazol-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(4-(2-hydroxypropan-2-yl)-1H-imidazol-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methyl-H-imidazol-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(2-methyl-H-imidazol-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrimidin-4(3H)-one,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrazin-2(1H)-one,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyridin-2(1H)-one,-   2-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ethanesulfonamide,-   2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)ethanesulfonamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methylaminosulfonamide,-   2-aminoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-hydroxyethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(2-oxopyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(2-oxopyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-((R)-3-hydroxypyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(piperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(piperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(4-methylpiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   2-(4-methylpiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   3-(2-aminoethyl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)imidazolidin-2-one,-   1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)imidazolidin-2-one,-   1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1H-imidazol-2(3H)-one,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)-1H-imidazol-2(3H)-one,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-(2-oxopyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(2-oxopyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-morpholinoethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethylpiperazine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(4-methylpiperazin-1-yl)ethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)morpholine-4-carboxamide,-   N-(2-aminoethyl)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,-   4-(3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylureido)butanoic    acid,-   N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)piperazine-1-carboxamide,-   N-(2-aminoethyl)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   1-((3R)-3-fluoropiperidin-4-yl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S)-3-fluoropiperidin-4-yl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((3R)-3-hydroxypiperidin-4-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((3S)-3-hydroxypiperidin-4-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((3R)-3-(hydroxymethyl)piperidin-4-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((3S)-3-(hydroxymethyl)piperidin-4-yl)urea,-   1-((3R)-3-(aminomethyl)piperidin-4-yl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S)-3-(aminomethyl)piperidin-4-yl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   3-((3R)-3-fluoropiperidin-4-yl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methylurea,-   3-((3S)-3-fluoropiperidin-4-yl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((3R)-3-hydroxypiperidin-4-yl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((3S)-3-hydroxypiperidin-4-yl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((2S)-2-(hydroxymethyl)piperidin-4-yl)urea,-   1-((2S)-2-(aminomethyl)piperidin-4-yl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((2R)-2-(hydroxymethyl)piperidin-4-yl)urea,-   1-((2R)-2-(aminomethyl)piperidin-4-yl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(piperidin-4-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-(2-hydroxyethyl)-3-(piperidin-4-yl)urea,-   1-(2-aminoethyl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(piperidin-4-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-((S)-piperidin-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((S)-piperidin-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-(2-hydroxyethyl)-3-((S)-piperidin-3-yl)urea,-   1-(2-aminoethyl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((S)-piperidin-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-((R)-piperidin-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((R)-piperidin-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-(2-hydroxyethyl)-3-((R)-piperidin-3-yl)urea,-   1-(2-aminoethyl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((R)-piperidin-3-yl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(piperidin-4-ylmethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-((R)-piperidin-2-ylmethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-((S)-piperidin-2-ylmethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((5-hydroxypiperidin-2-yl)methyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((5-hydroxypiperidin-2-yl)methyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((6-(hydroxymethyl)piperidin-2-yl)methyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-((6-(hydroxymethyl)piperidin-2-yl)methyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-((S)-piperidin-3-ylmethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-((R)-piperidin-3-ylmethyl)urea,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)-1,4-diazepane-1-carboxamide,-   N-(2-aminoethyl)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-(2-aminoethyl)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,89,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-3-oxopiperazine-1-carboxamide,-   (S)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-1-carboxamide,-   (R)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-1-carboxamide,-   (S)-3-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-1-carboxamide,-   (R)-3-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-1-carboxamide,-   (R)-3-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   (S)-3-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(4-methyl-2-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)-1-methylurea,-   2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylacetamide,-   N-((3S,5R,89,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5R,89,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-2-morpholinoacetamide,-   N-((3S,5R,89,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)-2-morpholinoacetamide,-   N-(2-aminoethyl)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-morpholinoacetamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpropanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpropanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)propanamide,-   (S)-2-amino-N-(2-aminoethyl)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   (R)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N1-methylsuccinamide,-   (S)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N1-methylsuccinamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-3-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-3-carboxamide,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(methylsulfonamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(2-(pyrrolidin-1-yl)acetamido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(1-methylpyrrolidine-2-carboxamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-3-((methoxycarbonyl)amino)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-3-((methoxycarbonyl)(methyl)amino)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl((2-morpholinoethoxy)carbonyl)amino)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)ureido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(N-methylpiperazine-1-carboxamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3-(N,4-dimethylpiperazine-1-carboxamido)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(3-(piperidin-4-yl)ureido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(N-methyl-1,4-diazepane-1-carboxamido)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3-(N,4-dimethyl-1,4-diazepane-1-carboxamido)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methylpiperazin-1-yl)-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-morpholino-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-amino-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   4-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(piperidin-4-ylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   methyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-aminoethyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   2-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-morpholinoacetamide,-   (R)-2-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)-2-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)-2-amino-N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)-2-amino-N1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (S)-2-amino-N1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)succinamide,-   (S)—N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   N-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-((1-methylpiperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3R)-3-fluoropiperidin-4-yl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3S)-3-fluoropiperidin-4-yl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3R)-3-fluoropiperidin-4-yl)(methyl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3S)-3-fluoropiperidin-4-yl)(methyl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3R)-3-fluoro-1-methylpiperidin-4-yl)(methyl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3S)-3-fluoro-1-methylpiperidin-4-yl)(methyl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3R)-3-fluoro-1-methylpiperidin-4-yl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(((3S)-3-fluoro-1-methylpiperidin-4-yl)amino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(methyl(piperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((S)-3-(aminomethyl)morpholino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((R)-3-(aminomethyl)morpholino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((R)-3-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((S)-3-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((R)-2-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((S)-2-(aminomethyl)morpholino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((R)-2-(aminomethyl)morpholino)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((S)-2-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((S)-2-(hydroxymethyl)pyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((R)-2-(hydroxymethyl)pyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((S)-2-(aminomethyl)pyrrolidin-1-yl)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((R)-2-(aminomethyl)pyrrolidin-1-yl)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((S)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((S)-3-aminopyrrolidin-1-yl)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-((R)-3-aminopyrrolidin-1-yl)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((R)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-3-(1,4-diazepan-1-yl)-5,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(4-methyl-1,4-diazepan-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((R)-2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((S)-2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-(2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((S)-3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-((R)-3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-(3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   1-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-(1H-imidazol-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-3-(4-(2-hydroxypropan-2-yl)-1H-imidazol-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(4-methyl-1H-imidazol-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-3-(2-methyl-1H-imidazol-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   3-((3S,5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrimidin-4(3H)-one,-   2-(pyrrolidin-1-yl)ethyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-morpholinoethyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methylpyrrolidine-2-carboxamide,-   methyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,-   methyl    ((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethylpiperazine-1-carboxamide,-   1-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(piperidin-4-yl)urea,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethyl-1,4-diazepane-1-carboxamide,-   5-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperidin-1-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methylpiperazin-1-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholino-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholino-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((8R,9S,10R,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)methanesulfonamide,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-1-methylpyrrolidine-2-carboxamide,-   methyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)carbamate,-   methyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)(methyl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)(methyl)carbamate,-   2-morpholinoethyl    ((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)(methyl)carbamate,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-N-methylpiperazine-1-carboxamide,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-7-(N,4-dimethylpiperazine-1-carboxamido)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-(piperidin-4-yl)ureido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(N-methyl-1,4-diazepane-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-N,4-dimethyl-1,4-diazepane-1-carboxamide,-   5-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(piperidin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-1-yl)-2H-pyran-2-one,-   5-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(piperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-1-yl)-2H-pyran-2-one,-   5-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(4-methylpiperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-1-yl)-2H-pyran-2-one,-   5-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-morpholinohexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-1-yl)-2H-pyran-2-one,-   5-((1R,2aR,3aS,3bR,5aR,9aS,9bS,11aR)-9a,11a-dimethyl-7-(piperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-1-yl)-2H-pyran-2-one,-   5-((1R,2aR,3aS,3bR,5aR,9aS,9bS,11aR)-9a,11a-dimethyl-7-(pyrrolidin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-1-yl)-2H-pyran-2-one,-   N-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-N-methylmorpholine-4-carboxamide,-   1-((1R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-7-yl)-1-methyl-3-(2-(3-oxopiperazin-1-yl)ethyl)urea,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(methylsulfonamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(2-(pyrrolidin-1-yl)acetamido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(1-methylpyrrolidine-2-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-7-((methoxycarbonyl)amino)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-7-((methoxycarbonyl)(methyl)amino)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(methyl((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(methyl((2-morpholinoethoxy)carbonyl)amino)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(N-methylpiperazine-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-7-(N,4-dimethyl-1,4-diazepane-1-carboxamido)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(piperidin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(piperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(4-methylpiperazin-1-yl)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-morpholino-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(piperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,9aS,9bS,11aR)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(pyrrolidin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(N-methylmorpholine-4-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,11a-dimethyl-7-(1-methyl-3-(2-(3-oxopiperazin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(methylsulfonamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(2-(pyrrolidin-1-yl)acetamido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(1-methylpyrrolidine-2-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-7-((methoxycarbonyl)amino)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-7-((methoxycarbonyl)(methyl)amino)-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(methyl((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(methyl((2-morpholinoethoxy)carbonyl)amino)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(N-methylpiperazine-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-7-(N,4-dimethylpiperazine-1-carboxamido)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(3-(piperidin-4-yl)ureido)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(N-methyl-1,4-diazepane-1-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-7-(N,4-dimethyl-1,4-diazepane-1-carboxamido)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(piperidin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(piperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(4-methylpiperazin-1-yl)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-morpholino-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(piperazin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-1-(2-oxo-2H-pyran-5-yl)-7-(pyrrolidin-1-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(N-methylmorpholine-4-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   (1R,2R,2aR,3aS,3bR,5aS,7S,9aR,9bS,11aR)-5a-hydroxy-9a,11a-dimethyl-7-(1-methyl-3-(2-(3-oxopiperazin-1-yl)ethyl)ureido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-3-aminopyrrolidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-3-aminopyrrolidin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperidin-4-ylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl(piperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-(3-hydroxypiperidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-3-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-3-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-3-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-3-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-2-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-2-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-2-(hydroxymethyl)morpholino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-2-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-2-(aminomethyl)morpholino)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((R)-3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((S)-3-(hydroxymethyl)piperazin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((R)-3-(aminomethyl)piperazin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,13R,14S,17R)-3-((S)-3-(aminomethyl)piperazin-1-yl)-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   methyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-aminoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-hydroxyethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(3-oxopiperazin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   3-(2-aminoethyl)-1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-morpholinoethyl)urea,-   N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)piperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(hydroxymethyl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-1,4-diazepane-1-carboxamide,-   (S)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-1-carboxamide,-   (R)-3-hydroxy-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-1-carboxamide,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((S)-3-hydroxypyrrolidin-1-yl)ethyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-((R)-3-hydroxypyrrolidin-1-yl)ethyl)-1-methylurea,-   N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylacetamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpropanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpropanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   (R)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N1-methylsuccinamide,-   (S)-2-amino-N1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N1-methylsuccinamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-2-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-2-carboxamide,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-3-((R)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-3-((S)-3-hydroxypyrrolidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-(piperidin-4-ylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-(methyl(piperidin-4-yl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-3-(3-hydroxypiperidin-1-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   methyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-aminoethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-hydroxyethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   3-(2-aminoethyl)-1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)-1-methylurea,-   1-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-morpholinoethyl)urea,-   N-((5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,-   N-((5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-(2-hydroxyethyl)piperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-1,4-diazepane-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxy-N-methylpyrrolidine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxy-N-methylpyrrolidine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-morpholinoacetamide,-   2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,-   2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylacetamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpropanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpropanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,-   (R)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (S)-2-amino-N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,-   (R)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-2-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,12R,13S,14S,17R)-12,14-dihydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpyrrolidine-2-carboxamide,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(piperidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3-(N,4-dimethylpiperazine-1-carboxamido)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methyl-1,4-diazepan-1-yl)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(4-methylpiperazin-1-yl)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-morpholino-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(methylsulfonamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-3-((methoxycarbonyl)(methyl)amino)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-3-(((2-aminoethoxy)carbonyl)(methyl)amino)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-3-(((2-hydroxyethoxy)carbonyl)(methyl)amino)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl((2-(pyrrolidin-1-yl)ethoxy)carbonyl)amino)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(methyl((2-morpholinoethoxy)carbonyl)amino)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)ureido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(1-methyl-3-(2-morpholinoethyl)ureido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(N-methylpiperazine-1-carboxamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(N-methylpiperazine-1-carboxamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-3-(2-(pyrrolidin-1-yl)acetamido)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(N-methyl-2-(pyrrolidin-1-yl)acetamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(2-morpholinoacetamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   (3S,5R,8R,9S,10S,13R,14S,16S,17R)-14-hydroxy-10,13-dimethyl-3-(N-methyl-2-morpholinoacetamido)-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-16-yl    acetate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   methyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-morpholinoethyl)urea,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylmorpholine-4-carboxamide,-   N-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-4-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-1,4-diazepane-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-2-morpholinoacetamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   5-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-morpholino-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(piperidin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(pyrrolidin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(piperazin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(4-methyl-1,4-diazepan-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,17S)-3-(1,4-diazepan-1-yl)-10,13-dimethyl-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(piperazin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   5-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(4-methylpiperazin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,-   methyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-(pyrrolidin-1-yl)ethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   2-morpholinoethyl    ((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-(pyrrolidin-1-yl)ethyl)urea,-   1-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-1-methyl-3-(2-morpholinoethyl)urea,-   N-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,4-dimethylpiperazine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methyl-1,4-diazepane-1-carboxamide,-   (S)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxy-N-methylpyrrolidine-1-carboxamide,-   (R)—N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-hydroxy-N-methylpyrrolidine-1-carboxamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-(pyrrolidin-1-yl)acetamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)-2-morpholinoacetamide,-   N-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,-   4-((3S,5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(piperazin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(4-methylpiperazin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(piperazin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-morpholino-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,13R,17S)-10,13-dimethyl-3-(piperidin-1-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,13R,17S)-3-(1,4-diazepan-1-yl)-10,13-dimethyl-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   4-((5R,8R,9S,10S,12R,13S,14S,17R)-3-amino-12,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,-   (1R,2R,2aR,3aS,3bR,5aR,7S,9aS,9bS,11aR)-9a,117-dimethyl-7-(N-methylmorpholine-4-carboxamido)-1-(2-oxo-2H-pyran-5-yl)hexadecahydronaphtho[1′,2′:6,7]indeno[1,7a-b]oxiren-2-yl    acetate, and-   4-((5R,8R,9S,10-,13R,178)-0,13-dimethyl-3-(4-methyl-1,4-diazepan-7-yl)-2,3,4,5,6,7,8,9,10,11,12,13,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl)furan-2(5H)-one,    and pharmaceutically acceptable salts thereof.

Also provided is at least one chemical entity chosen from the compoundsset forth in Table 1 below and pharmaceutically acceptable saltsthereof.

TABLE 1 Illustrative Compounds of the Present Invention Compound No.Chemical Name C01N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide C02N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide C03N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide C04N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide C05N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide C06N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide C071-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea C081-(2-aminoethyl)-3-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea C091-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea C101-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea C112-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide C122-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide C13(S)-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide C14(S)-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide C155-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one C16N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide Chemical Formula: C25H37NO5S Exact Mass: 463.2Molecular Weight: 463.6 C17 methyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate C185-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one C194-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one C205-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one C21methyl ((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate C22(2R)-2-amino-N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide C23N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylmorpholine-4-carboxamide C24N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide C25(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide C26(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide C275-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one C285-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one C29(2R)-2-amino-N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide C30N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide C31(2R)-N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide C325-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one C33 2-morpholinoethyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate C345-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2- oneC35 5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2- one

The chemical entities described herein can be synthesized utilizingtechniques well known in the art from commercially available startingmaterials and reagents. For example, the chemical entities describedherein can be prepared as illustrated below with reference to theexamples and reaction schemes.

Generally, compounds of Formula I may be prepared by the routesdescribed below. Materials used herein are either commercially availableor prepared by synthetic methods generally known in the art. Theseschemes are not limited to the compounds listed or by any particularsubstituents, which are employed for illustrative purposes. Althoughvarious steps of are described and depicted in Schemes A-C, the steps insome cases may be performed in a different order than the order shown inSchemes A-C. Various modifications to these synthetic reaction schemesmay be made and will be suggested to one skilled in the art havingreferred to the disclosure contained in this Application. Numbering doesnot necessarily correspond to that of claims or other tables.

In Scheme A, alcohol A-1 is oxidized to ketone A-2 using an oxidizingagent such as Jone's reagent in acetone. A-2 is then under reductiveamination to afford A-3 in the presence of an amine and a reducing agentsuch as NaBH₃CN in a polar organic solvent such as MeOH. Separation oftwo diastereoisomers using silica gel chromatography or HPLC afford A-4and A-5.

In Scheme B, B-1 is synthesized from ketone A-2 is converted to amineB-1 using reductive amination in the presence of an amine and a reducingagent such as NaBH₃CN in a polar organic solvent such as MeOH. B-1 canbe first separated to give two diastereoisomers B-2 and B-3, which canbe derivatized to afford corresponding B-5 and B-6 respectively. B-1 canalso be first derivatized to give B-4, which can be separated to affordB-5 and B-6.

Scheme C

In Scheme C, ketone A-2 is reduced to give alcohol C-1 as a mixture oftwo diastereoisomers in the presence of a reducing agent such as NaBH₄in a polar organic solvent such as MeOH or dioxane. The hydroxyl groupof C-1 is then converted to a leaving group such as tosyl (OTs), mesyl(OMs) or triflate (OTf). Displacement of the leaving group with amine orheteroaryl such as imidazole, pyrazole, or pyrimidin-4(3H)-one in thepresence a base affords C-3. Suitable bases include, but are not limitedto, Et₃N, pyridine, DMAP, Na₂CO₃, K₂CO₃, Cs₂CO₃, NaOMe, t-BuONa, t-BuOK,NaH, KH, LiH, and CaH₂. Suitable solvents include, but are not limitedto, DMF, DMSO, DMA, and N-methyl piperidone. The displacement reactionare generally carried out at a temperature ranging from 25-240° C. C-3can then be separated to afford two corresponding singlediastereoisomers. Alternatively, C-1 can be first separated to twosingle diastereoisomers, which can then be derivatized, displaced toafford the final compound of Formula I.

The desired product can be purified from the reaction mixture bystandard methods, e.g. by extraction and/or silica gel chromatography orhigh-pressure liquid chromatography.

The chemical entities described herein may be prepared in substantiallypure form, typically by standard chromatographic methods, prior toformulation in a pharmaceutically acceptable form.

The chemical entities described herein may be used in treating a varietyof cancers. Cancers that can be prevented and/or treated by the chemicalentities, compositions, and methods described herein include, but arenot limited to, human sarcomas and carcinomas, e.g. carcinomas, e.g.,colon carcinoma, pancreatic cancer, breast cancer, ovarian cancer,prostate cancer, fibrosarcoma, myxosarcoma, liposarcoma, chondrosarcoma,osteogenic sarcoma, chondroma, angiosarcoma, endotheliosarcoma,lymphangiosarcoma, lymphangioendotheliosarcoma, synovioma, mesothelioma,Ewing's tumor, leiomyosarcoma, rhabdomyosarcoma, squamous cellcarcinoma, basal cell carcinoma, adenocarcinoma, sweat gland carcinoma,sebaceous gland carcinoma, papillary carcinoma, papillaryadenocarcinomas, cystadenocarcinoma, medullary carcinoma, bronchogeniccarcinoma, renal cell carcinoma, hepatoma, bile duct carcinoma,choriocarcinoma, seminoma, embryonal carcinoma, Wilms' tumor, cervicalcancer, testicular tumor, lung carcinoma, small cell lung carcinoma,bladder carcinoma, epithelial carcinoma, glioma, astrocytoma,medulloblastoma, craniopharyngioma, ependymoma, pinealoma,hemangioblastoma, acoustic neuroma, oligodendroglioma, meningioma,melanoma, neuroblastoma, retinoblastoma, leukemias, e.g., acutelymphocytic leukemia and acute myelocytic leukemia (myeloblastic,promyelocytic, myelomonocytic, monocytic and erythroleukemia); chronicleukemia (chronic myelocytic (granulocytic) leukemia and chroniclymphocytic leukemia); and polycythemia vera, lymphoma (Hodgkin'sdisease and non-Hodgkin's disease), multiple myeloma, Waldenstrom'smacroglobulinemia, and heavy chain disease.

In some embodiments, the chemical entities described herein are used forthe treatment of cancers of the

(i) digestive system including, without limitation, the esophagus,stomach, small intestine, colon (including colorectal), liver &intrahepatic bile duct, gallbladder & other biliary, pancreas, and otherdigestive organs;

(ii) respiratory system, including without limitation, larynx, lung &bronchus, and other respiratory organs;

(iii) breast;

(iv) genital system, including without limitation, uterine cervix,ovary, and prostate;

(v) urinary system, including without limitation, urinary bladder andkidney and renal pelvis; and

(vi) oral cavity & pharynx, including without limitation, tongue, mouth,pharynx, and other oral cavity.

In some embodiments, the chemical entities described herein are used forthe treatment of colorectal cancer, liver cancer, lung cancer, breastcancer and oral cancer.

Chemical entities described herein having the desired pharmacologicalactivity may be administered, in some embodiments, as a pharmaceuticallyacceptable composition comprising an pharmaceutical excipient, to apatient, as described herein. Depending upon the manner of introduction,the chemical entities may be formulated in a variety of ways asdiscussed below. The concentration of the at least one chemical entityin the formulation may vary from about 0.01-100 wt. %.

The administration of the chemical entities described herein can be donein a variety of ways, including, but not limited to, orally,subcutaneously, intravenously, intranasally, transdermally,intraperitoneally, intramuscularly, intrapulmonary, vaginally, rectally,or intraocularly.

Pharmaceutical dosage forms include at least one chemical entitydescribed herein and one or more pharmaceutical excipients. As is knownin the art, pharmaceutical excipients are secondary ingredients whichfunction to enable or enhance the delivery of a drug or medicine in avariety of dosage forms (e.g.: oral forms such as tablets, capsules, andliquids; topical forms such as dermal, opthalmic, and otic forms;suppositories; injectables; respiratory forms and the like).Pharmaceutical excipients include inert or inactive ingredients,synergists or chemicals that substantively contribute to the medicinaleffects of the active ingredient. For example, pharmaceutical excipientsmay function to improve flow characteristics, product uniformity,stability, taste, or appearance, to ease handling and administration ofdose, for convenience of use, or to control bioavailability. Whilepharmaceutical excipients are commonly described as being inert orinactive, it is appreciated in the art that there is a relationshipbetween the properties of the pharmaceutical excipients and the dosageforms containing them.

Pharmaceutical excipients suitable for use as carriers or diluents arewell known in the art, and may be used in a variety of formulations.See, e.g., Remington's Pharmaceutical Sciences, 18th Edition, A. R.Gennaro, Editor, Mack Publishing Company (1990); Remington: The Scienceand Practice of Pharmacy, 21^(st) Edition, Lippincott Williams & Wilkins(2005); Handbook of Pharmaceutical Excipients, 3rd Edition, A. H. Kibbe,Editor, American Pharmaceutical Association, and Pharmaceutical Press(2000); and Handbook of Pharmaceutical Additives, compiled by Michaeland Irene Ash, Gower (1995), each of which is incorporated herein byreference for all purposes.

Oral solid dosage forms such as tablets will typically comprise one ormore pharmaceutical excipients, which may for example help impartsatisfactory processing and compression characteristics, or provideadditional desirable physical characteristics to the tablet. Suchpharmaceutical excipients may be selected from diluents, binders,glidants, lubricants, disintegrants, colors, flavors, sweetening agents,polymers, waxes or other solubility-retarding materials.

Compositions for intravenous administration will generally compriseintravenous fluids, i.e., sterile solutions of simple chemicals such assugars, amino acids or electrolytes, which can be easily carried by thecirculatory system and assimilated.

Dosage forms for parenteral administration will generally comprisefluids, particularly intravenous fluids, i.e., sterile solutions ofsimple chemicals such as sugars, amino acids or electrolytes, which canbe easily carried by the circulatory system and assimilated. Such fluidsare typically prepared with water for injection USP. Fluids usedcommonly for intravenous (IV) use are disclosed in Remington: TheScience and Practice of Pharmacy, Lippincott Williams & Wilkins (2005).The pH of such IV fluids may vary, and will typically be from 3.5 to 8as known in the art.

The chemical entities described herein may also be used in conjunctionwith other well known therapeutic agents that are selected for theirparticular usefulness against the condition that is being treated. Forexample, the chemical entities described herein may be useful incombination with at least one additional anti-cancer and/or cytotoxicagents. Further, the chemical entities described herein may also beuseful in combination with other inhibitors of parts of the signalingpathway that links cell surface growth factor receptors to nuclearsignals initiating cellular proliferation.

Such known anti-cancer and/or cytotoxic agents that may be used incombination with the chemical entities described herein include:

(i) other antiproliferative/antineoplastic drugs and combinationsthereof, as used in medical oncology, such as alkylating agents (forexample cis-platin, oxaliplatin, carboplatin, cyclophosphamide, nitrogenmustard, melphalan, chlorambucil, busulphan, temozolamide andnitrosoureas); antimetabolites (for example gemcitabine and antifolatessuch as fluoropyrimidines like 5-fluorouracil and tegafur, raltitrexed,methotrexate, cytosine arabinoside, and hydroxyurea); antitumorantibiotics (for example anthracyclines like adriamycin, bleomycin,doxorubicin, daunomycin, epirubicin, idarubicin, mitomycinC,dactinomycin and mithramycin); antimitotic agents (for example vincaalkaloids like vincristine, vinblastine, vindesine and vinorelbine andtaxoids like taxol and taxotere and polokinase inhibitors); andtopoisomerase inhibitors (for example epipodophyllotoxins like etoposideand teniposide, amsacrine, topotecan and camptothecin);

(ii) cytostatic agents such as antioestrogens (for example tamoxifen,fulvestrant, toremifene, raloxifene, droloxifene and iodoxyfene),antiandrogens (for example bicalutamide, flutamide, nilutamide andcyproterone acetate), LHRH antagonists or LHRH agonists (for examplegoserelin, leuprorelin and buserelin), progestogens (for examplemegestrol acetate), aromatase inhibitors (for example as anastrozole,letrozole, vorazole and exemestane) and inhibitors of 5a-reductase suchas finasteride;

(iii) anti-invasion agents [for example c-Src kinase family inhibitorslike4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4yloxyquinazoline(AZD0530; International Patent Application WO 01/94341),N-(2-chloro-6-methylphenyl)-2-{6-[4-(2-hydroxyethyl)piperazin-1-yl]-2-methylpyrimidin-4ylamino}thiazole-5-carboxamide(dasatinib, BMS-354825; J. Med. Chern., 2004, 47, 66586661) andbosutinib (SKI-606), and metalloproteinase inhibitors like marimastat,inhibitors of urokinase plasminogen activator receptor function orantibodies to Heparanase];

(iv) inhibitors of growth factor function: for example such inhibitorsinclude growth factor antibodies and growth factor receptor antibodies(for example the anti-erbB2 antibody trastuzumab [HERCEPTIN™], theanti-EGFR antibody panitumumab, the anti-erbB 1 antibody cetuximab[ERBITUX®, C225] and any growth factor or growth factor receptorantibodies disclosed by Stem et al. Critical reviews inoncology/haematology, 2005, Vol. 54, pp 11-29); such inhibitors alsoinclude tyrosine kinase inhibitors, for example inhibitors of theepidermal growth factor family (for example EGFR family tyrosine kinaseinhibitors such asN-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine(gefitinib, ZD1839),N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine(erlotinib, OSI-774) and6-acrylamido-N-(3-chloro-4-fluorophenyl)-7-(3-morpholinopropoxy)-quinazolin-4-amine(CI 1033), erbB2 tyrosine kinase inhibitors such as lapatinib);inhibitors of the hepatocyte growth factor family; inhibitors of theinsulin growth factor family; inhibitors of the platelet-derived growthfactor family such as imatinib and/or nilotinib (AMN107); inhibitors ofserine/threonine kinases (for example Ras/Raf signalling inhibitors suchas farnesyl transferase inhibitors, for example sorafenib (BAY 43-9006),tipifarnib (RI15777) and lonafarnib (SCH66336)), inhibitors of cellsignalling through MEK and/or AKT kinases, c-kit inhibitors, abl kinaseinhibitors, P13 kinase inhibitors, Plt3 kinase inhibitors, CSF-IR kinaseinhibitors, IGF receptor (insulin like growth factor) kinase inhibitors;aurora kinase inhibitors (for example AZD1152, PH739358, VX-680,MLN8054, R763, MP235, MP529, VX-528 and AX39459) and cyclin dependentkinase inhibitors such as CDK2 and/or CDK4 inhibitors;

(v) antiangiogenic agents such as those which inhibit the effects ofvascular endothelial growth factor, [for example the anti-vascularendothelial cell growth factor antibody bevacizumab (AVASTIN™) and forexample, a VEGF receptor tyrosine kinase inhibitor such as vandetanib(ZD6474), vatalanib (PTK787), sunitinib (SU11248), axitinib (AG-013736),pazopanib (GW 786034) and4.{4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3pyrrolidin-1-ylpropoxy)quinazoline(AZD2171; Example 240 within WO 00/47212), compounds such as thosedisclosed in International Patent Applications WO 97/22596, WO 97/30035,WO 97/32856 and WO 98/13354 and compounds that work by other mechanisms(for example linomide, inhibitors of integrin av˜3 function andangiostatin));

(vi) vascular damaging agents such as Combretastatin A4 and compoundsdisclosed in International Patent Applications WO 99/02166, WO 00/40529,WO 00/41669, WO 01/92224, WO 02/04434 and WO 02/08213;

(vii) an endothelin receptor antagonist, for example zibotentan (ZD4054)or atrasentan;

(viii) antisense therapies, for example those which are directed to thetargets listed above, such as ISIS 2503, an anti-ras antisense;

(ix) gene therapy approaches, including for example approaches toreplace aberrant genes such as aberrant p53 or aberrant BRCA1 or BRCA2,GDEPT (gene-directed enzyme pro-drug therapy) approaches such as thoseusing cytosine deaminase, thymidine kinase or a bacterial nitroreductaseenzyme and approaches to increase subject tolerance to chemotherapy orradiotherapy such as multi-drug resistance gene therapy; and

(x) immunotherapy approaches, including for example ex-vivo and in-vivoapproaches to increase the immunogenicity of subject's tumor cells, suchas transfection with cytokines such as interleukin 2, interleukin 4 orgranulocyte-macrophage colony stimulating factor, approaches to decreaseT-cell anergy, approaches using transfected immune cells such ascytokine-transfected dendritic cells, approaches usingcytokine-transfected tumor cell lines and approaches usinganti-idiotypic antibodies.

In certain embodiments, the at least one chemical entity is administeredin combination with one or more agents chosen from pacliataxel,bortezomib, dacarbazine, gemcitabine, trastuzumab, bevacizumab,capecitabine, docetaxel, erlotinib, aromatase inhibitors, such asAROMASIN™ (exemestane), and estrogen receptor inhibitors, such asFASLODEX™ (fulvestrant).

When a chemical entity described herein is administered into a humansubject, the daily dosage will normally be determined by the prescribingphysician with the dosage generally varying according to the age,weight, and response of the individual subject, as well as the severityof the subject's symptoms.

In one exemplary application, a suitable amount of at least one chemicalentity is administered to a mammal undergoing treatment for cancer, forexample, breast cancer. Administration typically occurs in an amount ofbetween about 0.01 mg/kg of body weight to about 100 mg/kg of bodyweight per day (administered in single or divided doses), such as atleast about 0.1 mg/kg of body weight per day. A particular therapeuticdosage can include, e.g., from about 0.01 mg to about 1000 mg of thechemical entity, such as including, e.g., from about 1 mg to about 1000mg. The quantity of the at least one chemical entity in a unit dose ofpreparation may be varied or adjusted from about 0.1 mg to 1000 mg, suchas from about 1 mg to 300 mg, for example 10 mg to 200 mg, according tothe particular application. The amount administered will vary dependingon the particular IC₅₀ value of the at least one chemical entity usedand the judgment of the attending clinician taking into considerationfactors such as health, weight, and age. In combinational applicationsin which the at least one chemical entity described herein is not thesole active ingredient, it may be possible to administer lesser amountsof the at least one chemical entity and still have therapeutic orprophylactic effect.

In some embodiments, the pharmaceutical preparation is in unit dosageform. In such form, the preparation is subdivided into unit dosescontaining appropriate quantities of the active component, e.g., aneffective amount to achieve the desired purpose.

The actual dosage employed may be varied depending upon the requirementsof the subject and the severity of the condition being treated.Determination of the proper dosage for a particular situation is withinthe skill of the art. Generally, treatment is initiated with smallerdosages which are less than the optimum dose of the at least onechemical entity. Thereafter, the dosage is increased by small amountsuntil the optimum effect under the circumstances is reached. Forconvenience, the total daily dosage may be divided and administered inportions during the day if desired.

The amount and frequency of administration of the at least one chemicalentities described herein, and if applicable other chemotherapeuticagents and/or radiation therapy, will be regulated according to thejudgment of the attending clinician (physician) considering such factorsas age, condition and size of the subject as well as severity of thedisease being treated.

The chemotherapeutic agent and/or radiation therapy can be administeredaccording to therapeutic protocols well known in the art. It will beapparent to those skilled in the art that the administration of thechemotherapeutic agent and/or radiation therapy can be varied dependingon the disease being treated and the known effects of thechemotherapeutic agent and/or radiation therapy on that disease. Also,in accordance with the knowledge of the skilled clinician, thetherapeutic protocols (e.g., dosage amounts and times of administration)can be varied in view of the observed effects of the administeredtherapeutic agents (i.e., antineoplastic agent or radiation) on thesubject, and in view of the observed responses of the disease to theadministered therapeutic agents.

Also, in general, the at least one chemical entities described hereinneed not be administered in the same pharmaceutical composition as achemotherapeutic agent, and may, because of different physical andchemical characteristics, be administered by a different route. Forexample, the chemical entities/compositions may be administered orallyto generate and maintain good blood levels thereof, while thechemotherapeutic agent may be administered intravenously. Thedetermination of the mode of administration and the advisability ofadministration, where possible, in the same pharmaceutical composition,is well within the knowledge of the skilled clinician. The initialadministration can be made according to established protocols known inthe art, and then, based upon the observed effects, the dosage, modes ofadministration and times of administration can be modified by theskilled clinician.

The particular choice of chemical entity (and where appropriate,chemotherapeutic agent and/or radiation) will depend upon the diagnosisof the attending physicians and their judgment of the condition of thesubject and the appropriate treatment protocol.

The chemical entities described herein (and where appropriatechemotherapeutic agent and/or radiation) may be administeredconcurrently (e.g., simultaneously, essentially simultaneously or withinthe same treatment protocol) or sequentially, depending upon the natureof the proliferative disease, the condition of the subject, and theactual choice of chemotherapeutic agent and/or radiation to beadministered in conjunction (i.e., within a single treatment protocol)with the chemical entity/composition.

In combinational applications and uses, the chemical entity/compositionand the chemotherapeutic agent and/or radiation need not be administeredsimultaneously or essentially simultaneously, and the initial order ofadministration of the chemical entity/composition, and thechemotherapeutic agent and/or radiation, may not be important. Thus, theat least one chemical entity described herein may be administered firstfollowed by the administration of the chemotherapeutic agent and/orradiation; or the chemotherapeutic agent and/or radiation may beadministered first followed by the administration of the at least onechemical entity described herein. This alternate administration may berepeated during a single treatment protocol. The determination of theorder of administration, and the number of repetitions of administrationof each therapeutic agent during a treatment protocol, is well withinthe knowledge of the skilled physician after evaluation of the diseasebeing treated and the condition of the subject. For example, thechemotherapeutic agent and/or radiation may be administered first, andthen the treatment continued with the administration of the at least onechemical entity described herein followed, where determinedadvantageous, by the administration of the chemotherapeutic agent and/orradiation, and so on until the treatment protocol is complete.

Thus, in accordance with experience and knowledge, the practicingphysician can modify each protocol for the administration of a chemicalentity/composition for treatment according to the individual subject'sneeds, as the treatment proceeds.

The attending clinician, in judging whether treatment is effective atthe dosage administered, will consider the general well-being of thesubject as well as more definite signs such as relief of disease-relatedsymptoms, inhibition of tumor growth, actual shrinkage of the tumor, orinhibition of metastasis. Size of the tumor can be measured by standardmethods such as radiological studies, e.g., CAT or MRI scan, andsuccessive measurements can be used to judge whether or not growth ofthe tumor has been retarded or even reversed. Relief of disease-relatedsymptoms such as pain, and improvement in overall condition can also beused to help judge effectiveness of treatment.

EXAMPLES

The following examples serve to more fully describe the manner of usingthe invention. These examples are presented for illustrative purposesand should not serve to limit the true scope of the invention.

In carrying out the procedures of the methods described herein, it is ofcourse to be understood that reference to particular buffers, media,reagents, cells, culture conditions and the like are not intended to belimiting, but are to be read so as to include all related materials thatone of ordinary skill in the art would recognize as being of interest orvalue in the particular context in which that discussion is presented.For example, it is often possible to substitute one buffer system orculture medium for another and still achieve similar, if not identical,results. Those of skill in the art will have sufficient knowledge ofsuch systems and methodologies so as to be able, without undueexperimentation, to make such substitutions as will optimally servetheir purposes in using the methods and procedures disclosed herein.

Examples 1 & 2: Preparation of5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(example 1) and5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(Example 2)

5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

To a suspension of5-((3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(5.25 g, 13.6 mmol, 1 eq.) in acetone (80 mL) at 0° C. was added Jone'sReagent (2.25 M, 6 mL, 1 eq.) dropwise. The resulting mixture wasstirred at 0° C. for 3 h. To the mixture was added NaHSO₃ in smallportions and the solution was extracted with DCM (3×50 mL). The combinedorganic phase was dried over anhydrous Na₂SO₄ and concentrated to afford5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(5.2 g, 98%).

To a suspension of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(5.2 g, 13.6 mmol, 1 eq.) in MeOH (100 mL) was added AcONH₄ (11.6 g,163.2 mmol, 12 eq.) followed by NaBH₃CN (1.71 g, 27.2 mmol 2 eq.). Afterbeing stirred at RT for 2 h, the mixture was added 1N HCl slowly to pH2, then basified to pH 9 by the addition of Na₂CO₃. The mixture wasextracted with DCM (3×50 mL). The combined organic layers were driedover anhydrous Na₂SO₄, concentrated and purified via prep-HPLC (10-40%CH₃CN in water with 0.1% TFA) to afford5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(R_(f)=3.9 min, 1.3 g, 50%) and5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(R_(f)=3.6 min, 710 mg, 27.2%). Analytical data for5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one:LRMS (M+H⁺) m/z calculated 386.3, found 386.2. ¹H NMR (CD₃OD, 400 MHz) δ7.99 (dd, 1H), 7.43 (d, 1H), 6.28 (d, 1H), 3.71 (t, 1H), 3.12-3.13 (m,1H), 2.54-2.58 (m, 1H), 2.14-2.22 (m, 2H), 1.12-1.96 (m, 21H), 0.98 (s,3H), 0.71 (s, 3H); Analytical data for5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one:LRMS (M+H⁺) m/z calculated 386.3, found 386.2. ¹H NMR (CDCl₃, 400 MHz) δ7.84 (dd, 1H), 7.24 (d, 1H), 6.26 (d, 1H), 3.27 (s, 1H), 2.46-2.48 (m,1H), 1.16-2.22 (m, 21H), 0.98 (s, 3H), 0.64 (s, 3H).

Example 3: Preparation of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

To a suspension of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(115 mg, 0.3 mmol, 1 eq.) in MeOH (10 mL) was slowly added pyrrolidine(420 mg, 6 mmol, 20 eq.), followed by NaBH₃CN (38 mg, 0.6 mmol, 2 eq.).The reaction mixture was adjusted to pH 6 by the addition of HOAc (2mL). After being stirred for 1 h at RT, the mixture was concentrated,basified to pH 9 by the addition of sat. Na₂CO₃ solution. The mixturewas extracted with DCM (3×50 mL). The combined organic layers were driedover anhydrous Na₂SO₄, concentrated and recrystallized from ethylacetate to afford5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(69.5 mg, 52.6%). LRMS (M+H⁺) m/z calculated 440.3, found 440.4. ¹H NMR(CDCl₃, 400 MHz) δ 7.82-7.85 (m, 1H), 7.22 (d, 1H), 6.26 (d, 1H),2.44-2.70 (m, 5H), 2.10-2.19 (m, 3H), 1.55-2.05 (m, 12H), 1.04-1.52 (m,12H), 0.92 (d, 3H), 0.68 (d, 3H).

Example 4: Preparation of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(7.9 mg) was prepared as described for5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one.LRMS (M+H⁺) m/z calculated 455.3, found 455.4. ¹H NMR (CDCl₃, 400 MHz) δ7.84-7.87 (m, 1H), 7.23 (d, 1H), 6.26 (d, 1H), 2.85-2.89 (m, 4H),2.08-2.47 (m, 8H), 1.66-1.82 (m, 13H), 1.04-1.52 (m, 12H), 0.92 (s, 3H),0.70 (s, 3H).

Example 5: Preparation of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-(pyrrolidin-1-yl)ethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(33 mg) was prepared as described for5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one.LRMS (M+H⁺) m/z calculated 483.4, found 483.4. ¹H NMR (CDCl₃, 400 MHz) δ7.82-7.85 (m, 1H), 7.22 (d, 1H), 6.26 (d, 1H), 2.70 (t, 2H), 2.60 (t,2H), 2.50 (m, 6H), 2.05-2.15 (m, 3H), 1.77-1.86 (m, 9H), 1.17-1.54 (m,15H), 0.92 (d, 3H), 0.70 (d, 3H).

Example 6: Preparation of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-morpholinohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(45.9 mg) was prepared as described for5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one.LRMS (M+H⁺) m/z calculated 456.3, found 456.4. ¹H NMR (CDCl₃, 400 MHz) δ7.82-7.85 (m, 1H), 7.24 (d, 1H), 6.26 (d, 1H), 3.98-4.02 (m, 4H), 3.68(t, 2H), 2.82 (d, 6H), 2.47 (t, 1H), 1.87-2.14 (m, 6H), 1.40-1.61 (m,14H), 0.92 (d, 3H), 0.70 (d, 3H).

Example 7: Preparation of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-((2-morpholinoethyl)amino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(96 mg) was prepared as described for5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one.LRMS (M+H⁺) m/z calculated 499.3, found 499.4. ¹H NMR (CDCl₃, 400 MHz) δ7.82-7.85 (m, 1H), 7.22 (d, 1H), 6.26 (d, 1H), 3.71 (t 4H), 2.73 (t,2H), 2.46-2.52 (m, 7H), 2.05-2.15 (m, 2H), 1.67-1.86 (m, 6H), 1.16-1.59(m, 16H), 0.92 (d, 3H), 0.70 (d, 3H).

Example 8: Preparation of4-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one

4-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one

4-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazin-2-one(115 mg) was prepared as described for5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one.LRMS (M+H⁺) m/z calculated 469.3, found 469.4. ¹H NMR (CDCl₃, 400 MHz) δ7.82-7.88 (m, 1H), 7.23 (d, 1H), 6.26 (d, 1H), 5.84-5.89 (m, 1H),3.29-3.38 (m, 3H), 2.77-2.79 (m, 1H), 2.45-2.47 (m, 1H), 2.04-2.19 (m,3H), 1.66-1.89 (m, 9H), 1.04-1.60 (m, 14H), 0.92 (d, 3H), 0.70 (d, 3H).

Example 9: Preparation of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one

5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-3-((2-hydroxyethyl)(methyl)amino)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(15.4 mg) was prepared as described for5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(pyrrolidin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one.LRMS (M+H⁺) m/z calculated 444.3, found 444.4. ¹H NMR (CDCl₃, 400 MHz) δ7.83 (dd, 1H), 7.23 (s, 1H), 6.26 (d, 1H), 3.55-3.60 (m, 2H), 2.60-2.63(m, 1H), 2.44-2.48 (m, 3H), 2.29-2.19 (m, 4H), 2.06-2.18 (m, 1H),1.66-1.86 (m, 5H), 1.71-1.55 (m, 16H), 0.91-0.92 (m, 3H), 0.70 (s, 3H).

Example 10: Preparation ofN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide

N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide

To a solution of CDI (50 mg, 0.31 mmol, 4 eq.) and DIEA (24 mg, 0.19mmol, 2.4 eq.) in DCM (2 mL) was added5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(30 mg, 0.078 mmol, 1 eq.) and the resulting mixture was stirred at RTfor 1h. Then the mixture was added piperizine (376 mg, 3.9 mmol, 50 eq.)and the resulting mixture was stirred at RT overnight. The solid wasremoved by filtration and the filtrate was purified by prep-HPLC toaffordN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide(13.8 mg, 35%). LRMS (M+H⁺) m/z calculated 498.3, found 498.3. ¹H NMR(CDCl₃, 400 MHz) δ 7.81-7.84 (dd, 1H), 7.22-7.23 (s, 1H), 6.25-6.27 (d,1H), 4.24-4.26 (d, 1H), 3.67-3.68 (m, 1H), 3.31-3.34 (m, 4H), 2.85-2.88(m, 4H), 2.44-2.48 (m, 1H), 2.04-2.20 (m, 2H), 1.10-1.88 (m, 20H), 0.92(s, 3H), 0.70 (s, 3H).

Example 11: Preparation ofN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide

N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide

N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide(30.6 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 498.3, found 498.3. ¹H NMR (CDCl₃, 400 MHz) δ7.82-7.85 (dd, 1H), 7.22-7.23 (s, 1H), 6.25-6.27 (d, 1H), 4.63-4.64 (d,1H), 4.13 (m, 1H), 3.31-3.34 (m, 4H), 2.86-2.88 (m, 4H), 2.45-2.49 (m,1H), 1.08-2.22 (m, 22H), 0.96 (s, 3H), 0.70 (s, 3H).

Example 12: Preparation ofN-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide

N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide

N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(5-oxo-2,5-dihydrofuran-3-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide(16.6 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 486.3, found 486.4. ¹H NMR (CD₃OD, 400 MHz) δ5.93 (s, 1H), 5.04-5.09 (m, 1H), 4.96-4.97 (m, 1H), 3.58-3.99 (m, 1H),3.33-3.41 (m, 4H), 2.80-2.88 (m, 5H), 2.19-2.27 (m, 2H), 1.12-2.10 (m,20H), 0.99-1.01 (m, 3H), 0.91 (s, 3H).

Example 13: Preparation ofN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide

N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide

N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide(10.6 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 483.3.3, found 483.3. ¹H NMR (CDCl₃, 400 MHz)δ 7.82-7.85 (dd, 1H), 7.22-7.23 (s, 1H), 6.25-6.27 (d, 1H), 3.99-4.01(m, 1H), 3.68 (m, 1H), 3.30-3.33 (m, 4H), 2.44-2.48 (m, 1H), 1.10-2.20(m, 27H), 0.96 (s, 3H), 0.70 (s, 3H).

Example 14: Preparation ofN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide

N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide

N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide(3.5 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 483.3, found 483.3. ¹H NMR (CDCl₃, 400 MHz) δ7.81-7.84 (dd, 1H), 7.22-7.23 (s, 1H), 6.25-6.27 (d, 1H), 4.63-4.65 (d,1H), 4.13 (m, 1H), 3.70-3.72 (m, 4H), 3.32-3.34 (m, 4H), 2.45-2.49 (m,1H), 1.07-2.22 (m, 22H), 0.87 (s, 3H), 0.70 (s, 3H).

Example 15: Preparation of1-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea

1-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea

1-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea(12.1 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 473.3, found 473.3. ¹H NMR (DMSO-d6, 300 MHz)δ 7.91-7.95 (dd, 1H), 7.52 (s, 1H), 6.29 (d, 1H), 5.84 (d, 1H),5.65-5.96 (t, 1H), 4.61-4.65 (t, 1H), 4.16 (s, 1H), 3.31-3.38 (q, 3H),3.01-3.06 (q, 2H), 1.11-1.78 (m, 20H), 0.86 (s, 3H), 0.60 (s, 3H).

Example 16: Preparation of1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea

1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea

1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea(21.8 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 473.3, found 473.2. ¹H NMR (DMSO-d6, 400 MHz)δ 7.91-7.95 (dd, 1H), 7.52 (d, 1H), 6.28 (d, 1H), 6.18 (d, 1H), 5.82(brs, 1H), 4.09-4.17 (m, 1H), 3.81-3.85 (m, 1H), 3.35-3.38 (t, 2H),3.01-3.05 (m, 2H), 2.43-2.51 (m, 2H), 1.11-2.08 (m, 20H), 0.89 (s, 3H),0.60 (s, 3H).

Example 17: Preparation of1-(2-aminoethyl)-3-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea

1-(2-aminoethyl)-3-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea

1-(2-Aminoethyl)-3-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea(14.8 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 472.3, found 472.3. ¹H NMR (DMSO-d6, 300 MHz)δ 7.93 (d, 1H), 7.53 (s, 1H), 6.29 (d, 1H), 5.68-5.78 (m, 2H), 4.16 (s,1H), 2.91-2.98 (q, 2H), 2.44-2.53 (m, 2H), 1.96-2.07 (m, 2H), 1.01-1.79(m, 20H), 0.86 (s, 3H), 0.60 (s, 3H).

Example 18: Preparation of1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea

1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea

1-(2-Aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea(10.9 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 472.3, found 472.1. ¹H NMR (DMSO-d6, 300 MHz)δ 7.91-7.94 (dd, 1H), 7.70 (brs, 1H), 7.52 (s, 1H), 6.27-6.33 (m, 2H),5.98-6.01 (t, 1H), 4.14 (s, 1H), 3.83-3.87 (m, 1H), 3.16-3.24 (q, 2H),2.80-2.84 (q, 2H), 2.43-2.50 (m, 2H), 1.05-2.08 (m, 22H), 0.89 (s, 3H),0.60 (s, 3H).

Example 19: Preparation of 2-morpholinoethyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate

2-morpholinoethyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate

2-Morpholinoethyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate(25.8 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide.LRMS (M+H⁺) m/z calculated 543.3, found 543.4. ¹H NMR (CD₃OD, 400 MHz) δ7.89 (dd, 1H), 7.33 (d, 1H), 6.17-6.19 (d, 1H), 4.07-4.08 (m, 2H), 3.78(m, 1H), 3.59-3.61 (m, 4H), 2.44-2.55 (m, 7H), 1.16-2.09 (m, 22H), 0.88(s, 3H), 0.61 (s, 3H).

Example 20: Preparation ofN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide

N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide

To a solution of5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(50 mg, 0.13 mmol, 1 eq.) in DCM (2 mL) was added DIEA (50 mg, 0.39mmol, 3 eq.) followed by morpholine-4-carbonyl chloride (23 mg, 0.16mmol, 1.2 eq.) and the resulting mixture was stirred at RT overnight.The reaction mixture was concentrated and purified via flash columnchromatography to affordN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide(18.2 mg, 28% yield). LRMS (M+H⁺) m/z calculated 499.3, found 499.3. ¹HNMR (CDCl₃, 400 MHz) δ 7.83 (dd, 1H), 7.22-7.23 (s, 1H), 6.26 (d, 1H),4.25 (d, 1H), 3.65-3.70 (m, 5H), 3.32-3.34 (m, 4H), 2.44-2.48 (m, 1H),2.02-2.22 (m, 2H), 1.10-1.88 (m, 20H), 0.87 (s, 3H), 0.70 (s, 3H).

Example 21: Preparation ofN-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide

N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide

N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide(18.8 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide.LRMS (M+H⁺) m/z calculated 499.3, found 499.3. ¹H NMR (CDCl₃, 400 MHz) δ7.81-7.84 (dd, 1H), 7.22-7.23 (s, 1H), 6.25-6.27 (d, 1H), 4.63-4.65 (d,1H), 4.13 (m, 1H), 3.70-3.72 (m, 4H), 3.32-3.34 (m, 4H), 2.45-2.49 (m,1H), 1.07-2.22 (m, 22H), 0.87 (s, 3H), 0.70 (s, 3H).

Example 22: Preparation ofN-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide

N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide

N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide(9.1 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide.LRMS (M+H⁺) m/z calculated 515.3, found 515.3. ¹H NMR (CDCl₃, 400 MHz) δ7.81 (dd, 1H), 7.24 (d, 1H), 6.27 (d, 1H), 4.17 (s, 1H), 3.66-3.69 (t,4H), 3.31 (t, 4H), 2.47-2.51 (m, 1H), 2.17-2.25 (m, 2H), 1.99-2.07 (m,2H), 1.20-1.94 (m, 18H), 0.91 (s, 3H), 0.71 (s, 3H).

Example 23: Preparation of methyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate

methyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamateMethyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate

(18.2 mg) was prepared as described forN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide.LRMS (M+H⁺) m/z calculated 462.2, found 462.3. ¹H NMR (CDCl₃, 400 MHz) δ7.83 (dd, 1H), 7.23 (d, 1H), 6.26 (d, 1H), 4.95 (d, 1H), 3.94-3.97 (m,1H), 3.68 (s, 1H), 2.24-2.49 (m, 1H), 1.06-2.21 (m, 22H), 0.94 (s, 3H),0.70 (s, 3H).

Example 24: Preparation ofN-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide

N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide

To a solution of5-((3S,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(20 mg, 0.052 mmol, 1.0 eq.) in DCM (5 mL) was added DIEA (13.0 mg, 0.10mmol, 2.0 eq.) at 0° C., followed by methanesulfonyl chloride (8.9 mg,0.078 mmol, 1.5 eq.). After being stirred at RT for 1 h, the resultingmixture was evaporated and the residue was purified by flashchromatography (PE/EA=1:2, v/v) to affordN-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide(13.0 mg, 54%). LRMS (M−H⁺) m/z calculated 462.2, found 462.3. ¹H NMR(CDCl₃, 400 MHz) δ 7.82 (dd, 1H), 7.23 (d, 1H), 6.27 (d, 1H), 4.52 (d,1H), 3.79-3.85 (m, 1H), 2.97 (s, 1H), 2.44-2.49 (m, 1H), 2.16-2.22 (m,1H), 1.87-2.06 (m, 3H), 1.13-1.79 (m, 18H), 0.96 (s, 3H), 0.70 (s, 3H).

Example 25: Preparation ofN-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylmorpholine-4-carboxamide

N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N-methylmorpholine-4-carboxamide

To a suspension of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-oxohexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(1.0 g, 2.6 mmol, 1 eq.) in MeOH (50 mL) was added 30% MeNH2 solution inMeOH (968 mg, 31.2 mmol, 12 eq.), followed by NaBH₃CN (656 mg, 20.8 mmol8 eq.). After being stirring at RT for 2 h, the mixture was basified topH=9 by the addition of Na₂CO₃. The mixture was extracted with DCM (3×50mL). The combined organic layers were dried over anhydrous Na₂SO₄, andconcentrated to afford crude5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(700 mg, 67%) which was used directly in the next step.

To a solution of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(40 mg, 0.1 mmol, 1 eq.) in DCM (3 mL) was added DIEA (38.7 mg, 0.3mmol, 3 eq.), followed by morpholine-4-carbonyl chloride (22.5 mg, 0.15mmol, 1.5 eq.). The resulting mixture was stirred at RT overnight, thenconcentrated. The residue was purified via flash chromatography(PE/EA=1:2, v/v) to affordN-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide(20.1 mg, 39%). LRMS (M+H⁺) m/z calculated 513.3, found 513.3. ¹H NMR(CDCl₃, 400 MHz) δ 7.84 (dd, 1H), 7.23 (s, 1H), 6.26 (d, 1H), 3.66-3.70(m, 5H), 3.18-3.34 (m, 4H), 2.76 (d, 3H), 2.45-2.49 (m, 1H), 2.18-2.22(m, 1H), 1.08-2.07 (m, 20H), 0.93 (s, 3H), 0.70 (s, 3H).

Example 26: Preparation of methyl((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate

methyl((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate

To a solution of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(50 mg, 0.125 mmol, 1 eq.) and DIEA (48.3 mg, 0.375 mmol, 3 eq.) in DCM(100 mL) was added methyl carbonochloridate (17.6 mg, 0.18 mmol, 1.5eq.). After being stirred at RT for 2 h, the mixture was washed withsat. Na₂CO₃ solution (20 mL) and extracted with DCM (3×20 mL). Thecombined organic layers were dried over anhydrous Na₂SO₄, andconcentrated. The residue was purified by prep-HPLC to afford methyl((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate(22.8 mg, 38.4%). LRMS (M+H⁺) m/z calculated 458.3, found 458.3. ¹H NMR(CDCl₃, 400 MHz) δ 7.86 (dd, 1H), 7.24 (s, 1H), 6.27 (d, 1H), 3.95 (s,1H), 3.69-3.70 (m, 3H), 2.81-2.95 (m, 5H), 2.45-2.49 (m, 1H), 1.05-2.23(m, 21H), 0.96 (s, 3H), 0.71 (s, 3H).

Example 27: Preparation of2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide

2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide

To a solution of 2-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)aceticacid (11.6 mg, 0.039 mmol) in DCM (3 mL) was added SOCl₂ (46 mg, 0.39mmol, 10 eq.). The resulting mixture was stirred under reflux for 3 h,then concentrated in vacuo. The residue was dissolved in DCM (3 mL) andwas added to a mixture of5-((3R,5R,8R,9S,10S,13R,14S,17R)-3-amino-14-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(10 mg, 0.026 mmol, 0.66 eq.) in a mixture of DCM (3 mL) and saturatedaqueous NaHCO₃ solution (3 mL). The resulting mixture was stirred at RTfor 3 h and extracted with DCM (3×10 mL). The combined organic layerswere dried over MgSO₄ and purified by prep-HPLC to afford(9H-fluoren-9-yl)methyl(2-(((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)amino)-2-oxoethyl)carbamateas a white solid (7.6 mg, 44%).

To a solution of (9H-fluoren-9-yl)methyl(2-(((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)amino)-2-oxoethyl)carbamate(45 mg, 0.068 mmol, 1 eq.) in DCM (3 mL) was added piperidine (5 drops)and the resulting mixture was stirred at RT overnight. The reactionmixture was concentrated and purified by prep-HPLC to afford2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamideas a white solid (10.2 mg, 34%). LRMS (M+H⁺) m/z calculated 443.3, found443.2. ¹H NMR (CD₃OD, 400 MHz) δ 7.99 (dd, 1H), 7.43 (d, 1H), 6.28 (d,1H), 3.67 (t, 1H), 3.37 (s, 2H), 2.54-2.57 (m, 1H), 0.96-2.24 (m, 24H),0.91 (s, 3H), 0.70 (s, 3H).

Example 28: Preparation of2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide

2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide

2-Amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide(20.6 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 443.3, found 443.3. ¹H NMR (CD₃OD, 400 MHz) δ7.99 (dd, 1H), 7.43 (d, 1H), 6.28 (d, 1H), 4.16 (s, 1H), 3.56 (s, 2H),2.54-2.58 (m, 1H), 0.96-2.24 (m, 24H), 0.90 (s, 3H), 0.70 (s, 3H).

Example 29: Preparation of(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide

(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide

(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide(11.5 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 485.3, found 485.4. ¹H NMR (CD₃OD, 400 MHz) δ7.94 (dd, 1H), 7.38 (d, 1H), 6.23 (d, 1H), 4.06 (m, 1H), 3.12 (d, 1H),2.51 (m, 1H), 1.20-2.10 (m, 22H), 0.86-0.94 (m, 29H), 0.66 (s, 3H).

Example 30: Preparation of(2R)-2-amino-N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide

(2R)-2-amino-N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide

(2R)-2-amino-N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide(9.3 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 501.3, found 501.4. ¹H NMR (CDCl₃, 400 MHz) δ8.24 (d, 1H), 7.82 (dd, 1H), 7.24 (d, 1H), 6.27 (d, 1H), 4.28 (s, 1H),3.14 (brs, 1H), 2.31-2.51 (m, 1H), 1.90-2.29 (m, 7H), 1.20-1.87 (m,18H), 0.97 (d, 3H), 0.92 (s, 3H), 0.89 (d, 3H), 0.71 (s, 3H).

Example 31: Preparation of(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide

(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide

(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide(12.9 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 457.3, found 457.4. ¹H NMR (CD₃OD, 400 MHz) δ7.89 (dd, 1H), 7.34 (d, 1H), 6.18 (d, 1H), 3.98 (s, 1H), 3.38 (q, 1H),2.41-2.51 (m, 1H), 1.15-2.18 (m, 24H), 0.89 (s, 3H), 0.61 (s, 3H).

Example 32: Preparation of(S)—N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide

(S)—N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide

(S)—N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide(16.4 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 483.3, found 483.3. ¹H NMR (CD₃OD, 400 MHz) δ7.99 (dd, 1H), 7.43 (d, 1H), 6.28 (d, 1H), 4.55 (brs, 1H), 3.96 (t 1H),3.68-3.72 (m, 1H), 3.14-3.31 (m, 2H), 2.53-2.58 (m, 1H), 2.10-2.34 (m,3H), 1.06-1.98 (m, 24H), 0.89 (s, 3H), 0.61 (s, 3H).

Example 33: Preparation of(S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide

(S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide

(S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide(7.4 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 483.3, found 483.3. ¹H NMR (CD₃OD, 400 MHz) δ7.89 (dd, 1H), 7.33 (d, 1H), 6.18 (d, 1H), 4.04-4.07 (m, 2H), 3.15-3.26(m, 2H), 2.44-2.47 (m, 1H), 2.26-2.32 (m, 1H), 1.10-2.12 (m, 27H), 0.82(s, 3H), 0.62 (s, 3H).

Example 34: Preparation of(2R)—N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide

(2R)—N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide

(2R)—N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide(7.2 mg) was prepared as described for2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide.LRMS (M+H⁺) m/z calculated 499.3, found 499.3. ¹H NMR (CDCl₃, 400 MHz) δ8.49 (d, 1H), 7.82 (dd, 1H), 7.25 (d, 1H), 6.27 (d, 1H), 4.23-4.25 (m,1H), 3.81-3.85 (m, 1H), 3.02-3.06 (m, 2H), 2.01-2.51 (m, 9H), 1.31-1.98(m, 20H), 0.93 (s, 3H), 0.71 (s, 3H).

Example 35: Preparation of(2R)-2-amino-N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide

(2R)-2-amino-N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide

To a solution of5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(methylamino)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one(50 mg, 0.125 mmol, 1 eq.) in a mixture of sat. NaHCO₃ (10 mL) solutionand DCM (10 mL) was added (S)-(9H-fluoren-9-yl)methyl(1-chloro-3-methyl-1-oxobutan-2-yl)carbamate (64 mg, 0.18 mmol, 1.5 eq.)at 0° C. After being stirred at RT for 2 h, the mixture was washed withsat. Na₂CO₃ (10 mL) solution and extracted with DCM (3×20 mL). Thecombined organic layers were dried over anhydrous Na₂SO₄ andconcentrated. The residue was purified via flash column chromatography(PE/EA=1:2, v/v) to afford (9H-fluoren-9-yl)methyl((2R)-1-(((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)amino)-3-methyl-1-oxobutan-2-yl)carbamate(78 mg, 86%).

To a solution of (9H-fluoren-9-yl)methyl((2R)-1-(((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)amino)-3-methyl-1-oxobutan-2-yl)carbamate(78 mg, 0.11 mmol, 1 eq.) in DCM (3 mL) was added piperidine (8 drops).After being stirred at r.t overnight, the reaction mixture wasconcentrated and purified by Prep-HPLC to afford(2R)-2-amino-N-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-N,3-dimethylbutanamide(10.8 mg, 20%). LRMS (M+H⁺) m/z calculated 499.3, found 499.4. ¹H NMR(CD₃OD, 400 MHz) δ 7.89 (dd, 1H), 7.33 (s, 1H), 6.18 (d, 1H), 5.39 (s,1H), 2.81-2.99 (m, 3H), 2.07-2.08 (m, 1H), 1.21-2.07 (m, 26H), 0.85-0.94(m, 9H), 0.61 (s, 3H).

Example 36: Measurement of Equilibrium Solubility

The equilibrium solubility of compounds was measured in aqueous buffer.Excess amount of solid compound was added into buffer solution and thesample was briefly sonicated and then shaken at rt for 24 h. The samplewas filtered and the concentration was analyzed by HPLC UV. A standardsolution at 0.2 mg/mL was prepared in methanol or acetonitrile for eachcompound and used as an external standard for quantification. Data forrepresentative compounds in NaOAc/AcOH buffer (100 mM, pH 5.0) are shownin Table 2. The scale utilized in Tables 2 is as follows: +++ greaterthan 1 mg/mL; ++ between 1 and 0.1 mg/mL; and + less than 0.1 mg/mL.

TABLE 2 Solubility of several illustrative compounds SolubilityCompounds +++ C04, C10, C12, C18, C20, C22, C24, C26, C27, C28 ++ C19,C30 + C02, C32

Example 37: Inhibition of Cancer Cell Growth by Compounds Using MTTAssay

Inhibition of cell growth by compounds was measured using MTT assay(Mosmann, T., Journal of Immunological Methods, 1983, 65, 55-63). Tumorcell lines were purchased from ATCC (American Type Culture Collection,Manassas, Va.). All cell lines were maintained in RPMI 1640 (Hyclone)supplemented with 10% fetal bovine serum (FBS, Hyclone), glutamine (2mM, Hyclone), and antibiotics (penicillin 100 U/mL and streptomycin 50μg/mL) at 37° C. in a humidified atmosphere of 5% CO₂ in air. Taxol (asa positive control, Sigma) and compounds were dissolved in DMSO (Sigma),and the final concentration of DMSO in the medium was 1%. Tumor cellswere plated in 96-well plates at densities of about 4000 cells/well of a96-well plate and allowed to adhere/grow for 24 h. They were thentreated with various concentrations of drug for 72 h.3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT,Sigma) was used to determine the number of viable cells at the time ofcompound addition and the number of cells remaining after 72 h compoundexposure. The number of cells remaining after 72 h was compared to thenumber of viable cells at the time of compound addition by measuring theabsorbance at 570 nm, allowing for the calculation of growth inhibition.

All concentrations of compounds were tested in triplicate and controlswere averaged over 4 wells. IC₅₀ was calculated by plotting theconcentration of compound vs the percentage of inhibition in treatedwells using GraphPad Prism 5. Data for representative compounds areshown below. Table 3 shows IC₅₀ values of several compounds of theinvention against A549 cells. The scale utilized in Table 3 is asfollows: ++++ less than 20 nM; +++ between 20 nM and 100 nM; ++ between100 nM and 1000 nM; and + greater than 1000 nM.

TABLE 3 IC₅₀ of several illustrative compounds in A549 cells IC₅₀Compounds ++++ C02, C03, C04, C06, C10, C12, C14, C15, C16, C17, C20,C21, C25, C26, C27, C29, C31, C35 +++ C09, C11, C19, C22, C24, C30 ++C01, C05, C07, C08, C13, C18, C23, C28, C32 + C34

Example 38: Inhibition of Tumor Growth in Xenograft Model

Cells were implanted in BALB/c female nude mice and grown as tumorxenografts. When tumors achieved 120-200 mm³, mice were assigned intotreatment and control groups using randomized block design based upontheir tumor volumes. Each group contained 6 tumor-bearing mice. Tumorswere measured twice weekly in two dimensions using a caliper, and thetumor volume was calculated from two-dimensional measurements using theequation V=0.5×a×b² where a and b are the long and short diameters ofthe tumor, respectively. Relative tumor volume (RTV) was defined asTV_(t)/TV_(i), the ratio of the volume on a given day (TV_(t)) and thevolume at the start of treatment (TV_(i)). Relative tumor growth rate(T/C) was defined as RTV_(T)/RTV_(C), the ratio of relative tumor volumeof treatment group (RTV_(T)) and relative tumor volume of control group(RTV_(C)) on a given day. Inhibition of tumor growth in a A549 tumorxenograft model is shown below in Table 4 for a compound of Table 1.

TABLE 4 In vivo activity of an illustrative compound in A549 tumor modelTumor Volume Tumor Volume Dose Pre-treatment Post-treatment Compound(mg/kg) Schedule Route (mm³) (mm³) T/C Vehicle — qd X 21 i.v. 279 2083 —Compound 2 qd X 21 i.v. 278 1238 60%** **p < 0.01

While some embodiments have been shown and described, variousmodifications and substitutions may be made thereto without departingfrom the spirit and scope of the invention. For example, for claimconstruction purposes, it is not intended that the claims set forthhereinafter be construed in any way narrower than the literal languagethereof, and it is thus not intended that exemplary embodiments from thespecification be read into the claims. Accordingly, it is to beunderstood that the present invention has been described by way ofillustration and not limitations on the scope of the claims.

What is claimed is:
 1. A compound selected from the group consisting of:N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide;N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide;N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide;N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide;1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea;1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea;2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide;2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide;(S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide;5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one;N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide;methyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate;methyl((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate;(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide;(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide;N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide;and (2R)—N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide;or a pharmaceutically acceptable salt thereof.
 2. The compound of claim1, wherein the compound is:N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,or a pharmaceutically acceptable salt thereof.
 3. The compound of claim1, wherein the compound is: N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,or a pharmaceutically acceptable salt thereof.
 4. The compound of claim1, wherein the compound is: N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)piperazine-1-carboxamide,or a pharmaceutically acceptable salt thereof.
 5. The compound of claim1, wherein the compound is:N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-1-carboxamide,or a pharmaceutically acceptable salt thereof.
 6. The compound of claim1, wherein the compound is:1-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-(2-hydroxyethyl)urea,or a pharmaceutically acceptable salt thereof.
 7. The compound of claim1, wherein the compound is:1-(2-aminoethyl)-3-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)urea,or a pharmaceutically acceptable salt thereof.
 8. The compound of claim1, wherein the compound is:2-amino-N-((3R,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,or a pharmaceutically acceptable salt thereof.
 9. The compound of claim1, wherein the compound is:2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)acetamide,or a pharmaceutically acceptable salt thereof.
 10. The compound of claim1, wherein the compound is:(S)—N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,or a pharmaceutically acceptable salt thereof.
 11. The compound of claim1, wherein the compound is: 5-((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-3-(piperazin-1-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)-2H-pyran-2-one,or a pharmaceutically acceptable salt thereof.
 12. The compound of claim1, wherein the compound is:N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)methanesulfonamide,or a pharmaceutically acceptable salt thereof.
 13. The compound of claim1, wherein the compound is: methyl((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)carbamate,or a pharmaceutically acceptable salt thereof.
 14. The compound of claim1, wherein the compound is: methyl((5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)(methyl)carbamate,or a pharmaceutically acceptable salt thereof.
 15. The compound of claim1, wherein the compound is:(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)-3-methylbutanamide,or a pharmaceutically acceptable salt thereof.
 16. The compound of claim1, wherein the compound is:(R)-2-amino-N-((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)propanamide,or a pharmaceutically acceptable salt thereof.
 17. The compound of claim1, wherein the compound is:N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)morpholine-4-carboxamide,or a pharmaceutically acceptable salt thereof.
 18. The compound of claim1, wherein the compound is:(2R)—N-((5S,8R,9S,10R,13R,14S,17R)-5,14-dihydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl)pyrrolidine-2-carboxamide,or a pharmaceutically acceptable salt thereof.
 19. A pharmaceuticalcomposition comprising a pharmaceutically acceptable carrier and thecompound or pharmaceutically acceptable salt of claim
 1. 20. A method ofameliorating symptoms or slowing progression of lung cancer in asubject, the method comprising administering to the subject in needthereof a therapeutically effective amount of the compound orpharmaceutically acceptable salt of claim 1.